MEDISunday, 28 August 2005

7:00 PM-9:00 PM Washington DC Convention Center -- Hall A, Poster
Poster Session
Sponsored by Eli Lilly
Organizer:David Rotella
6H-Benzo[c]chromen-6-one derivatives as selective ERβ agonists
Wanying Sun, Lovji D. Cama, Elizabeth Birzin, Sudha Warrier, Louis Locco, Ralph Mosley, Milton M. Hammond, Susan P. Rohrer
4,8-Disubstituted 2-phenyl-quinolines as potent and selective estrogen receptor β ligands
An T. Vu, Stephen T. Cohn, Eric S. Manas, Heather A. Harris, Richard E. Mewshaw
4-Hydroxy-N-phenyl substituted phthalimides as selective estrogen receptor beta (ERb) ligands
John W. Ullrich, Robert R. Singhaus Jr., Raymond Unwalla, Heather A. Harris
Synthesis and deuterium-labeling of pure SERM acolbifene (EM-652.HCl, SCH 57068.HCl) glucuronides
Jean-yves Sancéau, Denis Larouche, Brigitte Caron, Patrick Bélanger, Agnčs Coquet, Alain Bélanger, Sylvain Gauthier, Fernand Labrie
Dihydrobenzoxathiin SERAMs: Discovery of an optimized antagonist side chain and application of novel side chains to existing SERM platforms
Timothy A. Blizzard, Frank DiNinno, Jerry D. Morgan II, Helen Y. Chen, Jane Y. Wu, Seongkon Kim, Wanda Chan, Elizabeth T. Birzin, Yi Tien Yang, Lee Yuh Pai, Edward C. Hayes, Carolyn A. DaSilva, Ralph T. Mosley, Paula M.D. Fitzgerald, Nandini Sharma, Susan P. Rohrer, James M. Schaeffer, Milton L Hammond
Discovery of tissue-selective osteoanabolic SARMs
Jiabing Wang, Carol A. McVean, David B. Whitman, Mark E. Duggan
New ligands for estrogen receptors
Jelena M. Janjic, Miranda Sarachine, Claire Coleman, Peter Wipf, Billy W. Day
Discovery of (4-phenylsulfanyl-phenoxy)-acetic acids as a novel class of PPARδ agonists
Rajiv Sharma, Jonathan Houze, Joshua Gergely, Michelle Akerman, Frank Kayser, Jean Danao, Jurgen Lehmann
Design, synthesis, and SAR of indane acetic acid derivatives: A new class of dual PPAR alpha/gamma agonists
Hai-Jun Zhang, Neil Bifulco, Ken Boakye, William Bullock, Thomas Claus, Philip Coish, Miao Dai, Fernado E. Dela Cruz, David Dickson, Ann Gore-Willse, Dongping Fan, Helena Hoover-Lilly, Tindy Li, Derek B. Lowe, Margit MacDougall, Gretchen Mannelly, Mary-Katherine Monahan, Ingo Mugge, Stephen O'Connor, Mareli Rodriguez, Tatiana Shelekhin, Laurel Sweet, Andreas Stolle, Ming Wang, Yamin Wang, Chengzhi Zhang, Kake Zhao, Qian Zhao, Jian Zhu, Manami Tsutsumi, Robert Schoenleber
6-(Arylamino)-4,4-disubstituted-1-methyl-1,4-dihydro-benzo[d][1,3]oxazin-2-ones as nonsteroidal progesterone receptor antagonists
Jeffrey C. Kern, Eugene A. Terefenko, Andrew Fensome, Ray J Unwalla, Jay Wrobel, Zhiming Zhang, Yun Zhu, Jeffrey Cohen, Richard Winneker, Puwen Zhang
Stable analogs of retinamides derived from TTNPB
Victoria V. Abzianidze, Michael D. Collins, Nirca J. Nieves, Margaret Clagett-Dame, Robert W. Curley Jr.
Synthesis of novel heterocyclic amino acids and their incorporation into somatostatin analogs
Audrey Kelleman, Michael S. VanNieuwenhze, Murray Goodman
New macrocycles as high affinity antagonists to the motilin receptor
Eric Marsault, Sylvie Beaubien, Kamel Benakli, Robert Déziel, Graeme Fraser, Hamid R. Hoveyda, Annick Landry, Luc G. Ouellet, Mark L. Peterson, Carl Saint-Louis, Martin Vézina, Zhigang Wang
Rotational barriers in the peripheral benzodiazepine receptor ligand, PK 11195: Determination by quantum chemistry and NMR
Victor W. Pike, Emmanuelle Briard, Fabrice G. Siméon, H. Umesha Shetty, Yong-Sok Lee
Aminopyrimidines as neuroprotective agents
Tina Morgan Ross, Robert Zivin, Paul Burnett, Malcolm K. Scott, Elfrida Grant, Douglas E. Brenneman, Allen B. Reitz
Excitatory amino acid transporters (EAATs): II. Identification of potent and selective EAAT-2 inhibitors
Alexander Greenfield, Cristina Grosanu, John Dunlop, Beal McIlvain, Tikva Carrick, Brian Jow, Qiang Lu, Dianne Kowal, Kristi Fan, John P Williams, John A. Butera
Excitatory amino acid transporters (EAATs): I. The search for selective EAAT modulators
John A. Butera, Alexander Greenfield, Cristina Grosanu, John Dunlop, H. Beal McIlvain, Tikva Carrick, Brian Jow, Qiang Lu, Dianne Kowal, John P Williams
Discovery and SAR of imidazo[1,2-b][1,2,4]triazines as GABAA α2/3 subtype selective agonists for the treatment of anxiety
Michael G. N. Russell, Robert W. Carling, Leslie J. Street, Richard T. Lewis, Andrew Mitchinson, Andrew S. R. Jennings, Melissa Hinch, John R. Atack, Susan M. Cook, Frances Bromidge, Keith A. Wafford, George R. Marshall, David S. Reynolds, Joanna Stanley, Rachael Lincoln, Spencer Tye, Wayne Sheppard, Bindi Sohal, Andrew Pike, Maria Dominguez, José L. Castro
Neuroprotective effects of EGIS-11229, a 2,3-benzodiazepine type AMPA antagonist
József Barkóczy, István Ling, Gyula Simig, Gábor Gigler, Annamária Simó, Angela Benedek, Krisztina Móricz, Márta Ágoston, Miklós Végh, Gábor Kapus, Szabolcs Kertész, György Lévay, László Hársing, Gábor Szénási
Derivatives to improve the oral bioavailability and subsequent plasma and brain levels of [2-(8,9-dioxo-2,6-diaza-bicyclo[5.2.0]non-1(7)-en-2-yl)-ethyl]-phosphonic acid (EAA-090, perzinfotel), a competitive NMDA antagonist
Reinhardt B. Baudy, John A. Butera, Jean Sze, Hong Chen, Uday Jain, Matthew Hoffmann, Michael K. May, Michael R. Brandt
Pharmacokinetic and pharmacodyamic effects of an oxymethylene-spaced diphenylester derivative of perzinfotel (EAA-090: [2-(8,9-Dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)-ethyl]phosphonic acid) in inflammatory and neuropathic pain models
Reinhardt B. Baudy, Hong Chen, Uday Jain, Christine Huselton, Cheryl Mugford, Rana Ramdass, Hamza Kandoussi, Michael R. Brandt, Jeffrey D. Kennedy
Synthesis and discovery 3-amino piperidine and pyrolidine-based inhibitors of neurotransmitter re-uptake transporters
Manuel Cases, John J. Masters, Louise Haughton, Gordon Campbell, Teresa Mann, Helene Rudyk, Magnus W. Walter, Graham Timms, Jeremy Gilmore, David R. Dobson, Craig White, John R. Boot, Jeremy D. Findlay, Lorna Hayhurst, Ann Helene Kluge, Sivi Mahadevan, Francoise J. Brunelle, Claude L. Delatour, Annie A. Lavis, Kenneth W. Perry, Frank P. Bymaster, Linda Thompson, Susan Hemrick-Luecke
Discovery of novel (2,4,5)-trisubstituted asymmetric pyran derivatives exhibiting selective affinity for the norepinephrine transporter: Importance of regioselectivity and stereoselectivity in binding activity, Part-I
Shijun Zhang, Juan Zhen, Maarten Reith, Aloke Dutta
Further structural exploration of novel (2,4,5)-trisubstituted asymmetric pyran derivatives: Exploration of different N-benzyl substitutions on activity for monoamine transporters, Part-II
Shijun Zhang, Fernando Fernandez, Juan Zhen, Maarten Reith, Aloke Dutta
Synthesis of an easily 18F-labeled and high affinity candidate radioligand for PET imaging of brain mGluR5 receptors
Fabrice G. Siméon, Velvet M. Patterson, Frederick T. Chin, Robert B. Innis, Victor W. Pike
Discovery and biological profile of a new class of metabotropic receptor 1 allosteric antagonist
Satoru Itoh, Atsushi Satoh, Yasushi Nagatomi, Yukari Hirata, Gentaroh Suzuki, Toshifumi Kimura, Akio Satow, Mikiko Hata, Hiroshi Kawamoto, Hisashi Ohta
Design and synthesis of novel mGluR5 antagonists
Santosh S Kulkarni, Barbara Nightingale, Christina M. Dersch, Richard B. Rothman, Amy Hauck Newman
Pyridazinone derived phenylalanine amides as alpha4 integrin antagonists
Yong Gong, Joseph K. Barbay, Alexey B. Dyatkin, Tamara A. Miskowski, Edward S. Kimball, Stephen M. Prouty, M. Carolyn Fisher, Rosemary Santulli, Craig R. Schneider, Nathaniel H. Wallace, John A. Masucci, William E. Hageman, Scott Ballentine, Dennis J. Hlasta, Pamela J. Hornby, Wei He
N-Ureido and N-carbamido pyridazinone-functionalized phenylalanines as alpha4beta7 integrin antagonists
Joseph K. Barbay, Yong Gong, Alexey B. Dyatkin, Tamara A. Miskowski, Edward S. Kimball, Stephen M. Prouty, M. Carolyn Fisher, Rosemary Santulli, Craig R. Schneider, Nathaniel H. Wallace, William E. Hageman, John A. Masucci, Scott Ballentine, Dennis J. Hlasta, Pamela J. Hornby, Wei He
Synthesis and biological studies of an integrin alpha-v-beta,5 guided therapeutic
Amir P. Tamiz, David C. Griffith, Teresa Aja, Lingna Li, Fang Liao, Krishnan Subbiah, Michael Whiney, Miriah Leclerc, Curt Bradshaw, Rodney Lappe, Sanjib Das, Subhash C. Sinha, Carlos F. Barbas III
Novel bivalent integrin antagonist compounds
Anand Francis, Christopher A. Burnett, Zhimin Shen, King C. P. Li, Narasimhan Danthi
Phenylalanine amide derivatives as alpha4 integrin antagonists
Tamara A. Miskowski, Alexey B. Dyatkin, Yong Gong, Joseph K. Barbay, M. Carolyn Fisher, Edward S. Kimball, Rosemary Santulli, Craig R. Schneider, Nathaniel H. Wallace, Scott Ballentine, Dennis J. Hlasta, Pamela J. Hornby, Wei He
Novel small-molecule antagonists of the chemokine receptor CXCR3
Marc-Raleigh Brescia, Andrew G. Cole, Ilana L. Stroke, Christopher Haskell, Sofia Ribeiro, Srilatha Simhadri, Joan J. Zhang, Zahid Hussain, Kenneth C. Appell, Ian Henderson, Maria L. Webb
Discovery and optimization of 2-aminothiazole derivatives as CCR4 antagonists
Xuemei Wang, Feng Xu, Qingge Xu, Hossen Mahmud, Jonathan Houze, Liusheng Zhu, Michelle Akerman, George Tonn, Liang Tang, Daniel J. Dairaghi, Tassie L. Collins, Julio C. Medina
Design, synthesis and structure-activity relationship studies of novel 4,4-disubstituted piperidine based CCR5 antagonists as anti-HIV-1 agents
Jennifer Peckham, Donald Anderson, Chris Aquino, Neil Bifulco, Larry Boone, Pek Chong, Maosheng Duan, Robert Ferris, Wieslaw Kazmierski, Terry Kenakin, Daniel G Lang, Ed McLean, Angilique Svolto, Patricia Wheelan, Michael Youngman
Mechanistic studies of novel voltage-gated sodium channel blockers as inhibitors of prostate cancer
Todd P. Hansen, Jill E. Lynch, Manoj K. Patel, Paulianda J. Griffith, Robert A. Sikes, Milton L. Brown
Chemical evolution of tricyclic antidepressants into novel monocyclic amines with potent sodium channel activity
Debjani P. Hudgens, Milton L. Brown, Cathy Taylor, Manoj K. Patel
Disjunctive approaches towards new steroidal sodium channel blockers based on a cholic acid scaffold
Gary C. Davis, Paulianda J. Griffith, Timothy Batts, Manoj Patel, Milton L. Brown
Comparative molecular field analysis and synthesis of novel sodium channel blockers from a combined phenytoin-lidocaine pharmacophore
Yuesheng Wang, Paulianda J. Griffith, James D. Anderson, Paul W Lenkowski, Victoria K. Landry, Manoj K Patel, Seong-Hoon Ko, Milton L. Brown
Identification and characterization of small molecule modulators of KChIP/Kv4 function
Lynne P. Greenblatt, Mark Bowlby, Pranab Chanda, Wade Edris, Joe Hinson, Flora Jow, Alan Katz, Girija Krishnamurthy, Keith Pitts, Kevin Ryan, Howard Zhang
Structure-activity relationship studies on diaminopyrimidines as growth hormone secretagogue receptor (GHS-R) antagonists
Bo Liu, Gang Liu, Mei Liu, Zhili Xin, Hongyu Zhao, Michael D. Serby, Christi Kosogof, Lissa TJ. Nelson, Bruce G. Szczepankiewicz, Wiweka Kaszubska, Verlyn G. Schaefer, Douglas H. Falls, Christine A. Collins, Hing L. Sham
Discovery of potent, selective and orally bioavailable growth hormone secretagogue receptor (Ghs-R) antagonists
Zhili Xin, Michael D. Serby, Hongyu Zhao, Mei Liu, Bo Liu, Charles W Hutchins, Kathy Sarris, Hoff Ethan, Douglas H Falls, Christine A. Collins, Chunwei Lin, Christopher A Ogiela, Michael E. Brune, Gene Bush, Brian Droz, Tom Fey, Vicki Knourek-Segel, Robin Shapiro, Peer Jacobson, David Beno, Teresa Turner, Hing L. Sham, Gang Liu
Diaminopyrimidines as growth hormone secretagogue receptor antagonists
Michael D. Serby, Gang Liu, Hongyu Zhao, Bruce G. Szczepankiewicz, Christi Kosogof, Wiweka Kaszubska, Douglas H. Falls, Verlyn G. Schaefer, Eugene N. Bush, Robin Shapiro, Brian A. Droz, Victoria E. Knourek-Segel, Thomas A. Fey, Michael E. Brune, David Beno, Teresa Turner, Christine A. Collins, Peer B Jacobson, Hing L. Sham
A-784168, a novel TRPV1 receptor antagonist as analgesic agent
Brian S. Brown, Guo Zhu Zheng, Robert G. Schmidt, Ryan G. Keddy, John R. Koenig, Tammie K Jinkerson, Heath A. McDonald, Minglei Cui, Prisca Honore, Kennan C. Marsh, John F. Darbyshire, Carol S. Surowy, Robert Moreland, Michael Jarvis, Connie R. Faltynek, Chih-Hung Lee
Novel, potent TRPV1 receptor antagonists
Brian S. Brown, Ryan G. Keddy, Guo Zhu Zheng, Robert G. Schmidt, John R. Koenig, Prisca Honore, Michael F. Jarvis, Carol S. Surowy, Connie R. Faltynek, Chih-Hung Lee
SAR of a new series of indole and indazole ureas as TRPV1 antagonists
Irene Drizin, Arthur Gomtsyan, Erol K. Bayburt, Richard J. Perner, Stanley Didomenico, John R. Koenig, Heath A. McDonald, Prisca Honore, Carol T. Wismer, Kennan Marsh, Jill Wetter, Michael F. Jarvis, Connie R. Faltynek, Chih-Hung Lee
4-(Pyridin-2-yl)-piperazine-N-cyano-1-carboxamidine analogs as vanilloid receptor 1 antagonists
Xiaoming Zhou, Qun Sun, Chongwu Zhang, Kenneth J. Valenzano, Jinchen Huang, Kevin C. Brown, Donald J. Kyle
Comparative protein structure modeling of the human Angiotensin II Type 1 (AT-1) receptor: Insights into the molecular determinants of the AT-1-ligand interactions
Akshay Patny, Prashant V. Desai, Mitchell A. Avery
N6-Ethyl-2-alkynyl adenosine derivatives as a selective human A3 adenosine receptor agonist
Ran Zhu, Cynthia R. Frazier, Timothy L. Macdonald, Joel Linden
Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-uronamides as human A3 adenosine receptor agonists
Lak Shin Jeong, Hyuk Woo Lee, Zhan-Guo Gao, Kenneth A. Jacobson, Dae Hong Shin, Jeong A Lee, Ae Yil Kim
Design, synthesis, and biological evaluation of novel adenosine A2A receptor antagonists
Lisa S. Silverman, John Caldwell, William J. Greenlee, Eugenia Y. Kiselgof, Julius Matasi, Deen Tulshian, Leyla Arik, Carolyn Foster
Biaryl and heteroaryl derivatives of SCH 58261 as potent and selective adenosine A2A receptor antagonists
Unmesh Shah, Craig D. Boyle, Samuel Chackalamannil, Bernard Neustadt, Carolyn Foster, Leyla Arik, Ying Zhai, Jean E. Lachowicz, Kwokei Ng, Shiyong Wang, Angela Monopoli, Ennio Ongini
(-)-Mefloquine as a starting point for the discovery of selective adenosine A2A receptor antagonists
Allan M. Jordan, Karen Benwell, Ian A. Cliffe, Colin T. Dourish, Paul R. Giles, Roger J. Gillespie, Tony R. Knight, Joanne Lerpiniere, A. Misra, Simon E. Ward, Scott M. Weiss
Human P2Y6 receptor: Molecular modeling and structure-based drug design
Stefano Costanzi, Pedro Besada, Bhalchandra V. Joshi, Savitri Maddileti, Liaman Mamedova, Dae Hong Shin, Maria J Gonzalez-Moa, Victor E. Marquez, T. Kendall Harden, Kenneth Jacobson
Synthesis and SAR of novel thieno[3,2-d]pyrimidine derivatives as selective antagonists of the adenosine A2A receptor
Allan M. Jordan, Ian A. Cliffe, Claire E. Dawson, Colin T. Dourish, Paul R. Giles, Roger J. Gillespie, Tony R. Knight, Anthony Lawrence, Joanne Lerpiniere, A. Misra, Robert M. Pratt, Richard S. Todd, Rebecca Upton, Scott M. Weiss
Uncharged isocoumarin-based inhibitors of urokinase-type plasminogen activator
Justin J. Heynekamp, Lucy A. Hunsaker, Lorraine M. Deck, David L. Vander Jagt
Synthesis of pyridoxal phosphate derivatives with antagonist activity at the P2Y13 receptor
Yong-Chul Kim, Jung-Sun Lee, Katrin Sak, Frederic Marteau, Liaman Mamedova, Jean-Marie Boeynaems, Kenneth A. Jacobson
Optimization of privileged structure for selective and potent melanocortin subtype-4 receptor ligands
Qingmei Hong, Raman K. Bakshi, Rui Tang, Rubana N. Kalyani, Tanya MacNeil, David H. Weinberg, Lex H. T. Van der Ploeg, Arther A. Patchett, Ravi Nargund
SAR and pharmocology of potent and selective melanocortin subtype-4 receptor agonists with azabicyclo carboxamide moiety
Liangqin Guo, Zhixiong Ye, Khaled J. Barakat, Patrick G. Pollard, Brenda L. Palucki, Iyassu K. Sebhat, Raman K. Bakshi, Rui Tang, Rubana N. Kalyani, Aurawan Vongs, Charles I. Rosenblum, Tanya MacNeil, David H. Weinberg, Qianping Peng, Constantin Tamvakopoulos, Randy R. Miller, Ralph A. Stearns, Erin McGowan, William J. Martin, Airu S. Chen, Joseph M. Metzger, Howard Y. Chen, Alison M. Strack, Euan MacIntyre, Lex H. T. Van der Ploeg, Matthew J. Wyvratt, Ravi P. Nargund
2-Aminoquinoline MCH1R antagonists: Structure-activity determinants and binding mode investigations
Trond Ulven, Thomas M. Frimurer, Jean-Marie Receveur, Paul Brian Little, Řystein Rist, Pia K. Nřrregaard, Thomas Högberg
4-Oxo-4H-chromene-2-carboxamides as melanin concentrating hormone antagonists: Structure-activity relationship of antiobesity therapeutics
Jennifer C. Freeman, John K. Lynch, Mathew M. Mulhern, Andrew S. Judd, Rajesh R. Iyengar, Gang Zhao, Sevan Brodjian, Doug Falls, Brian D. Dayton, Christopher A. Ogiela, Hanna E. Sidorowicz, Robin Shapiro, Victoria Knourek-Segel, Michael Brune, Sandra T. Leitza, Gilbert J. Diaz, Hing L. Sham, Christine A. Collins, Philip R. Kym
Discovery, lead optimization and in vivo studies on coumarin-based small molecule MCHr-1 antagonists
Rajesh R. Iyengar, Andrew J. Souers, John K. Lynch, Andrew S. Judd, Ju Gao, Jennifer C. Freeman, Mathew Mulhern, Anil Vasudevan, Dariusz Wodka, Christopher Blackburn, James Brown, Jennifer Lee Che, Courtney A. Luchaco-Cullis, Sujen Lai, Matthew J. Lamarche, Thomas H. Marsilje, Jonathan B. Roses, Bradley Geddes, Michael A. Patane, Dennis G. Fry, Brian D. Dayton, Sevan Brodjian, Doug H. Falls, Michael E. Brune, Eugene N. Bush, Robin Shapiro, Victoria E. Knourek-Segel, Thomas A. Fey, Cathleen A. McDowell, Thomas B. Farb, Glenn A. Reinhart, Lee C. Preusser, Kennan C. Marsh, Lisa E. Hernandez, James M. Schmidt, Hing L. Sham, Christine A. Collins, Philip R. Kym
Identification and SAR of hERG selective Melanin-concentrating hormone receptor 1 antagonists
Mathew M. Mulhern, Andrew Judd, Jennifer Freeman, John Lynch, Rajesh Iyengar, Andrew J. Souers, Ju Gao, Gang Zhao, Dariusz Wodka, Gilbert Diaz, Ruth Martin, Sevan Brodjian, Doug Falls, Brian Dayton, Hing L. Sham, Christine A. Collins, Philip R. Kym
Synthesis and structure activity relationship of biaryl cannabinoid mimetics: Phenol replacements
Q. Jean Zhou, Karin Worm, Roland E. Dolle, Gabriel Stabley, Robert N. DeHaven
Paper Withdrawn
Synthesis and biological evaluation of novel pyrido[3',2':4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT2C receptor agonists
Hans G. F. Richter, D. R. Adams, A. Benardeau, M. J. Bickerdike, J. M. Bentley, T. J. Blench, I. A. Cliffe, J. E. P. Davidson, C. Dourish, P. Hebeisen, G. A. Kennett, A. R. Knight, C. S. Malcolm, P. Mattei, A. Misra, J. Mizrahi, N. J. T. Monck, J-M. Plancher, S. Roever, J. R. A. Roffey, S. Taylor, S. P. Vickers
Development of dual-acting benzofurans and benzomorpholines as dual thromboxane A2 receptor antagonists and prostacyclin receptor agonists
Michihiro Ohno, Takahiro Takeda, Yoichiro Tanaka, Kei Makita, Mitsuko Miyamoto, Naohiro Yamada, Atsushi Ohtake
Pyrimidine substituted 2-phenyl-4-piperazinylbenzimidazole inhibitors of Gonadotropin Releasing Hormone
John F. Mehlmann, Jeffrey C. Pelletier, Joseph T. Lundquist IV, Joshua E. Cottom, Linda Shanno, Murty V. Chengalvala, Irene B. Feingold
Synthesis of 4’-carboxamido N-Boc-2’,6’-dimethyl-L-phenylalanines as surrogates for DMT in opioid receptor ligands
Chaozhong Cai, Henry J. Breslin, Tamara A. Miskowski, Sui-Po Zhang, Pamela Hornby, Wei He
Synthesis and SAR studies for 3,4-disubstituted oxyindoles as potent and selective antagonists of the EP3 receptor for PGE2
J Singh, N. Zhou, G Hategan, W Zeller, Lei Zhao, P Yu, L Enache, J Zhang, E Onua, J Ramirez, G Palsdottir, G Halldorsdottir, T Andersson, M Gurney
Synthesis, biological evaluation and metabolic stability of 3,4-disubstituted indoles as potent and selective EP3 receptor antagonists
J Singh, N Zhou, G Hategan, W Zeller, A Polozov, M Goldsmith, M Krohn, H Anderson, R Mishra, J Zhang, E Onua, J Ramirez, G Palsdottir, G Halldorsdottir, T Andresson, M Gurney
Discovery of novel aza-prostaglandin derivatives analogs of PGE2 as selective EP2 and EP4 receptors agonists
Gian Luca Araldi, Nadia Brugger, Bagna Bao, David Fischer, Srinivasa Karra, Sean McKenna, Yufang Xiao, Zhong Zhao
Structure-based design of a class of potent small molecule inhibitors of Bcl-2 and Bcl-xL proteins
Guozhi Tang, Zaneta Nikolovska-Coleska, Renxiao Wang, Jie Guo, Mei Lan Liu, Su Qiu, York Tomita, Shaomeng Wang
Discovery of novel orally active and selective ureido-NPY Y5 antagonists
Guoqing Li, Ying Huang, Joseph Kelly, Andrew Stamford, William Greenlee, Deborra Mullins, Mario Guzzi, Xiang Zhang, Joyce J. Hwa, Jun Gao, Lorraine Ghibaudi, Sam Weihaus, K-C. Cheng
Benzodiazepines as selective bradykinin B2 receptor antagonists
Carmen Leung, V. Santhakumar, Mirek Tomaszewski, Christopher Walpole, Simon Woo, Lynda Adam, Joanne Butterworth, Claude Godbout, Kemal Payza, Marie Roumi
Potent and selective BK-1 antagonists – 4-substituted phenyl cyclohexanes
John J. Lim, M. Kristine Markowitz, K.L. Murphy, S.S. O'Malley, R. W. Ransom, Ray S. Chang, D.J. Pettibone, R.M. Freidinger, M. G. Bock, D.S. Su
SAR of pyrrolidine containing H3 antagonists: Trends across multiple chemical series
Diana L Nersesian, Lawrence A Black, Thomas R Miller, Timothy A Esbenshade, Arthur A Hancock, Marlon D Cowart
Bicyclic heteroaromatic histamine H3 antagonists: Synthesis, potency, and in vivo profiles of analogs optimized for drug-likeness
Robert J. Altenbach, Huaqing Liu, Timothy A. Esbenshade, Gerard B. Fox, Arthur A Hancock, Marlon Cowart
Design, synthesis, and structure-activity relationship of novel non-imidazole histamine H3 antagonists
Huaqing Liu, Robert J. Altenbach, Thomas R. Miller, Timothy A. Esbenshade, Arthur A Hancock, Marlon Cowart
Discovery of novel natural alkaloid conessine as potent histamine H3 receptor antagonist
Chen Zhao, Y. L. Bennani, S. Gopalakrishnan, M. Sun, Timothy A. Esbenshade, K. M. Krueger, T. R. Miller, D. G. Witte, Kennan C. Marsh, Marlon D. Cowart, A. A. Hancock
Synthesis and pharmacological evaluation of selective, potent delta opioid agonists as novel analgesics
Andrea Penwell, Andrew Griffin, Paul Jones, Sylvain Bernard, Carmen Leung, Simon Woo, William Brown, Christopher Walpole, Maryse Labarre, Martin Coupal, Stéphane St-Onge, Lejla Hodzic, Dominic Salois, Kemal Payza
Rationale and synthesis of potent dual δ/μ opioid receptor ligands for motility disorders
Henry J. Breslin, Tamara A. Miskowski, Chaozhong Cai, Santosh V. Coutinho, Sui-Po Zhang, Pamela J. Hornby, Wei He
Synthesis and structure activity relationship of a series of 2- and 6-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists
Allan J. Goodman, Bertrand Le Bourdonnec, Mathieu Michaut, Hai Fen Ye, Thomas M. Graczyk, Serge Belanger, Robert N. DeHaven, Roland E. Dolle
Design, synthesis and biological evaluation of mu opioid selective biaryl-substitiuted 1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one derivatives
Alfonzo D. Jordan, Michael J. Orsini, Steven A. Middleton, Peter J. Connolly, Douglas E. Brenneman, Kevin Pan, Allen B. Reitz
Synthesis and evaluation of the benz[f]indene neurosteroid analogues
Jamie B Scaglione, Brad D. Manion, Alex S. Evers, Steven Mennerick, Charles F. Zorumski, Douglas F. Covey
NK1 Antagonists based on seven membered lactam scaffolds
Jason M Elliott, Emma J Carlson, Gary G. Chicchi, Olivier Dirat, Maria Dominguez, Ute Gerhard, Richard Jelley, A. Brian Jones, Marc M Kurtz, Kwei-lan Tsao, Alan Wheeldon
Design and synthesis of thrombin receptor antagonists
Martin Clasby, Samuel Chackalamannil, Michael Czarniecki, Dario Doller, Keith Eagen, William J. Greenlee, Grace Kao, Yan Lin, Hsingan Tsai, Yan Xia, Jacqueline Agans-Fantuzzi, Ho-Sam Ahn, George Boykow, Matthew Bryant, Madhu Chintala, Carolyn Foster, Janice Lau
Paper Withdrawn
Design and synthesis of arylsulfonyl thioureas as novel potent cyclophilin ligands
Larisa E. Serdyuk, Douglas E. Wilkinson, Sean K. Hamilton, Sergei A. Belyakov, Ling Wei, Bert E. Thomas IV, Gregory S. Hamilton, Edmond Massuda, Marigo Stathis, Mike Fuller, Camilo J. Rojas, Joseph P. Steiner, Shirley Huang, George Liu, Yong-Qian Wu
Design and synthesis of arylsulfonylthiosemicarbazides as potent, nonpeptidic cyclophilin inhibitors
Yong-Qian Wu, Douglas E. Wilkinson, Gregory S. Hamilton, Joseph Steiner, Sean Hamilton, Bert E. Thomas IV, Edmond Massuda, Mike Fuller, Marigo Stathis, Sergei A. Belyakov
Novel 1-(azacyclyl)-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines as 5-HT6 agonists and antagonists
Hassan Elokdah, Albert J. Robichaud, David Z. Li, Geraldine R. McFarlane, Ronald C. Bernotas, Gregory J. Tawa, Guo Ming Zhang, Deborah L. Smith, Lee E. Schechter
Novel 1-(2-aminoethyl)-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines as 5-HT6 agonists and antagonists
Ronald C. Bernotas, Steven Lenicek, Schuyler A. Antane, Guo Ming Zhang, Deborah L. Smith, Joseph Coupet, Lee E. Schechter
1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-pyrrolopyridines as novel 5-HT6 receptor ligands
Ronald C. Bernotas, Schuyler A. Antane, Steven Lenicek, Simon N. Haydar, Albert J. Robichaud, Guo Ming Zhang, Deborah L. Smith, Joseph Coupet, Lee E. Schechter
Spirocyclic indanes as ligands for the NOP (ORL-1) receptor
R. Richard Goehring, Xiaoming Zhou, Jin-Cheng Huang, Lisa J. Barnett, Qun Sun, Sam F. Victory, Kenneth J. Valenzano, Wendy S. Miller, Shen Shan, Donald J. Kyle
Development of predictive CoMFA and CoMSIA models for alkoxylated and hydroxylated chalcones as anti-malarial agents
Devendra Puntambekar, Mange Ram Yadav, Rajani Giridhar
A novel one-pot synthesis of thalidomide and its derivatives under microwave irradiation
Ellis Benjamin, Yousef Hijji
Design and synthesis of novel indole deivatives as anti-angiogenic agents
Sureyya Olgen, Dogu Nebioglu, Eiichi Akaho
Synthesis of radiolabeled 5-(aminomethyl)-2l-aminopyrrolo[2,3-d]pyrimidine-4(3H)-one (preQ1) and 2-amino-5-[(1S, 2R, 3S)-2, 3-dihydroxycyclopent-4-enylamino-methyl]pyrrolo[2, 3-d]pyrimidine-4(3H)-one (queuine)
Sureyya Olgen, George A. Garcia
Lipophilicity coefficients of new potential PET dopamine D2 and D3 receptor ligands (E)-4, 3, 2-[11C]methoxy-N-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)-cinnamoylamides and (E)-4, 3, 2-[18F]fluoro-N-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)-cinnamoylamides
Mingzhang Gao, Ji-Quan Wang, Qi-Huang Zheng
Synthesis of carbon-11 and fluorine-18 labeled 2-acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline analogues as new potential PET AMPA receptor ligands
Mingzhang Gao, Ji-Quan Wang, Qi-Huang Zheng
Development of [11C]MPT as a potential agonist PET tracer for 5-HT1A receptor imaging
Vattoly J Majo, Ramin V. Parsey, Hadassah Tamir, Matthew Millak, Shu-Chi Hsiung, Jaya Prabhakaran, Norman R. Simpson, Julie Arcement, Ronald L. Van Heertum, J. John Mann, J. S. Dileep Kumar
Synthesis and in vivo evaluation of [11C]MPM as a 5-HT2A receptor PET ligand
Jaya Prabhakaran, Ramin V. Parsey, Vattoly J Majo, Norman R. Simpson, Julie Arcement, Ronald L. Van Heertum, J. John Mann, J. S. Dileep Kumar
Synthesis of an iodine-123 labeled rofecoxib analogue: A potential SPECT agent
George W. Kabalka, Arjun R. Mereddy, Brandy Belue, Hildegard Schuller
Biotin derivatives for radiotherapeutics and fluorescent in vivo models
Shelly James, Kevin Maresca, John Valliant, John W. Babich, Laurie Doering, Jon Zubieta
Efficient deuterium labeling method of biologically active compounds
Hiroyoshi Esaki, Fumiyo Aoki, Tomohiro Maegawa, Hironao Sajiki, Kosaku Hirota
Facile and efficient isotope labeling method for phenylalanine derivatives catalyzed by Pd/C
Tomohiro Maegawa, Akira Akashi, Hiroyoshi Esaki, Fumiyo Aoki, Hironao Sajiki, Kosaku Hirota, Kenjiro Tatematsu, Yukio Mori
New effective tool for selecting optimal catalytic technology for chemical transformations
Johannes G. Donkervoort, James A. Schwindeman
Scale up synthesis of resolvin E1 and its bioaction
Tomomichi Chonan, Makoto Arita, Kiyoshi Takayama, Charles N. Serhan
Investigation of method evaluating the activities of SOD-like antioxidants using the whole synthesis-typed ROS sensor
Makoto Yuasa, Kenichi Oyaizu, Aritomo Yamaguchi, Seiko Ohseki, Tomohiro Kobayashi, Yuujiro Toyoda, Satoshi Tsutsui, Masahiro Nanba
Paper Withdrawn
Evaporative light scattering and polymeric SPE: A combined approach for compound repository analysis and clean up
Aubrey J Mendonca, Paul A Boguszewski, A F Coffey, John W Davies, A A MacDonald, F P Warner
Solid phase extraction of metals: Facile removal of active metal species prior to compound screening
Aubrey J Mendonca, Paul A Boguszewski, Andrew F Coffey, John W Davies, Alasdair A MacDonald, Frank P Warner
One-step scaffold hopping with novel synthetic strategies
László Ürge, Ákos Papp, Richard Jones, Norbert Varga, Ferenc Darvas
Diversity oriented synthesis(DOS) using poly-functional scaffolds
Eleanor F. Duffy, Mauro F. A. Adamo
Paper Withdrawn
Crystallization of pharmaceuticals on self-assembled monolayers on gold
Kasim Biyikli, Branko Zugic, Garrett P. Ebersole, Joshua B. Allor, John C. MacDonald
Nucleation and growth of polymorphs of pharmaceuticals on bulk substrates and in microfluidic channels with chemically modified surfaces
John C. MacDonald, Kasim Biyikli, Branko Zugic, Garrett P. Ebersole, Joshua B. Allor
Natural products analysis by new continuous polarity/volume gradient TLC
Yi-bo Guo, Qi-Feng Ma
Structural characterization and molecular investigation of a serendipitously discovered bioactive macromolecule, lignin sulfate
Arjun Raghuraman, Jay N. Thakkar, Gunnar Thor Gunnarsson, Michael Hindle, Umesh R. Desai
The role of planar chromatography in column purification
Jack Liu
The application of evaporative light scattering detection to high throughput HPLC methods
John A. McConville, S M Bullock
A protocol to accomplish "Homo-Robinson" annulation: Application to the guanacastepene problem
Heedong Yun, Samuel J. Danishefsky
Plusbacin A3: Efforts towards the solution phase synthesis
Aaron Wohlrab, Ryan Lamer, Michael S. VanNieuwenhze
Synthetic studies toward Nogalamycin
Ryan B. Lamer, Luis R. Rivera, Tristan Beaudette, Michelle Tetalman, Michael S. VanNieuwenhze
Synthesis of enone analogues of the natural product curcumin
Waylon M. Weber, Lucy A. Hunsaker, Lorraine M. Deck, David L. Vander Jagt
Synthesis and stereochemistry of epiquinamide
Richard W. Fitch, Gordon D. Sturgeon
A concise total synthesis of bromopyrrole alkaloid Manzacidin A
Hongfeng Chen, James C. Lanter, Xuqing Zhang, Zhihua Sui
A total synthesis of (-)-treprostinil using stereoselective Pauson Khand reaction
Kuanquiang Gao, Robert M. Moriarty, Jeffrey R. Deschamps
Synthesis of Sansalvamide A derivates
Joseph D. Brown, Ahmet Kekec, Shelli McAlpine
Studies towards the biomimetic synthesis of pyridomacrolidin
Nageswara R Irlapati, Jack E Baldwin, Robert M Adlington
Solvent-free synthesis of novel dihydropyrimidinones scaffolds
Qiang Yu, Fengping Wei, Liangfu Huang, Zhiqiang Fang, Wuping Ma
Recent progress on the synthesis and chemical-biological properties of nucleoside boranophosphate analogues
Ping Li, Mikhail I. Dobrikov, Hongyan Liu, Charlotta K. Wennefors, Barbara R. Shaw
Synthesis of ribo- and deoxyribonucleoside α-P-borano- and α-P-thiodiphosphates by a phosphoramidite approach
Zhihong Xu, Barbara Ramsay Shaw
Enantioselective carbolithiation cascade reaction for indole synthesis
Anne-Marie L. Hogan, Donal F. O'Shea
Synthesis of new GMII inhibitors, diversity-oriented 5-substituted swainsonine analogues, via stereoselective Mannich reaction
Shinichi Nakayama, Hideko Nagasawa, Tomoya Fujita, Toshihiro Hashimoto, Yoshinori Asakawa, Yoshihiro Uto, Hitoshi Hori, Douglas A. Kuntz
Development of efficient synthetic methods for chiral cyclopentenol derivatives using ring-closing metathesis (RCM) reaction and synthesis of unnatural neplanocin A (NPA) analogues
Jong-Hyun Cho, Chung K. Chu
Paper Withdrawn
Enantioselective synthesis of 2-substituted pipecolic acids and its application
Duen-ren Hou, Shin-Yi Hung, Chung-Cheng Hu
Synthesis and opioid binding affinity of (-)-octahydro-1H-benzofuro[3,2-e]isoquinolines
Ling-Wei Hsin, Li-Te Chang, C. M. Dersch, R. B. Rothman
Preparation and identification of pentostain isomers
Liping Gao, Wuyi Wang, Meizheng Liu
Indole inhibitors of cPLA2α: Synthetic routes
Richard Vargas, Katherine L. Lee, Mark L. Behnke, Lihren Chen, Wei Li, Paresh M. Thakker, Weiheng Wang, Fuk-Wah Sum, Alexander Oliphant, Kun Wu, Vishnu Hegde, Marina WH. Shen, John C. McKew
Carbocyclic N-3 isonucleosides as SAHase inhibitors for antiviral chemotherapeutics
Brian A. Bakke, Sylvester L. Mosley, Joshua M. Sadler, Narsesh K. Sunkara, Katherine L. Seley
Seldi proteinchip array analysis of hepatitis B virus infection and hepatocellular carcinoma
Rui Zhu, Qing-Yu He, Jen-Fu Chiu
Synthesis and in vitro anti-HCV screening of a series of ring-expanded ("fat") nucleosides containing the imidazo[4,5-e][1,3]diazepine-4,8-dione ring system
Peng Zhang, Ramachandra S. Hosmane
m-Tyrosine- and tic-based macrocyclic inhibitors of Hepatitis C Virus (HCV) NS3 protease: Synthesis and biological activity
Kevin X Chen, F. George Njoroge, John Pichardo, Andrew Prongay, Nancy Butkiewicz, Nanhua Yao, Vincent Madison, Viyyoor Girijavallabhan
Hepatitis C virus NS3 serine protease inhibitors: Discovery of potent P2’ moiety
Ashok Arasappan, F. G. Njoroge, T-Y. Chan, F. Bennett, S. L. Bogen, K. Chen, H. Gu, L. Hong, E. Jao, Y-T. Liu, R. G. Lovey, T. Parekh, R. E. Pike, P. Pinto, B. Santhanam, Srikanth Venkatraman, H. Vaccaro, H. Wang, X. Yang, Z. Zhu, N. Patel, J. McCormick, Brian McKittrick, A. K. Saksena, V. Girijavallabhan, J. Pichardo, N. Butkiewicz, R. Ingram, B. Malcolm, A. Prongay, N. Yao, B. Marten, V. Madison, S. Kemp, O. Levy, M. Lim-Wilby, S. Tamura, A. K. Ganguly
Novel 2-oxoimidazolidine-4-carboxylic acid derivatives as hepatitis C virus NS3 serine protease inhibitors
Ashok Arasappan, F. George Njoroge, Tejal N. Parekh, John Pichardo, Nancy Butkiewicz, Andrew Prongay, Nanhua Yao, Viyyoor Girijavallabhan
P2 Diamino acid derivatives as hepatitis C virus NS3 serine protease inhibitors
Ashok Arasappan, F. George Njoroge, Haining Gu, Tejal N. Parekh, John Pichardo, Nancy Butkiewicz, Andrew Prongay, Nanhua Yao, Viyyoor Girijavallabhan
Application of phenylphosphate mimetics to the design and synthesis of olefin metathesis-derived Grb2 SH2 domain-binding macrocycles
Terrence R Burke Jr., Sang Uk Kang, Won Jun Choi, Zhen-Dan Shi, Rajeshri Karki, Jason Phan, Karen M. Worthy, Lakshman Bindu, Marc C. Nicklaus, David S. Waugh, Robert J. Fisher
Design and synthesis of depeptidized P2-P4 biaryl macrocyclic inhibitors of hepatitis-C NS3-4A protease
Srikanth Venkatraman, F. George Njoroge, Viyyoor Girijavallabhan, V. Madison, N. Yao, Andrew Prongay, Nancy Butkiewicz, John Pichardo
Discovery of SCH6: A new ketoamide inhibitor of the HCV NS3 serine protease
Stephane Bogen, A. Arasappan, F. Bennett, T-Y. Chan, Kevin X Chen, S. Hendrata, L. Hong, H. Huang, Edwin Jao, Y-T. Liu, R. Lovey, J. McCormick, T. Parekh, R. E. Pike, Patrick Pinto, S. Ruan, B. Santhanam, S. Venkatraman, H. Vaccaro, B. Vibulbhan, H. Wang, Z. Zhu, Brian McKittrick, F. G. Njoroge, A. K. Saksena, V. Girijavallabhan, B. Baroudy, N. Butkiewicz, A. Hart, R. Liu, B. Malcolm, J. Pichardo, D. Standring, A. Prongay, N. Yao, V. Madison, S. Kemp, O. Levy, M. Lim-Wilby, S. Tamura, A. K. Ganguly
Synthesis and structure-activity relationship of P3-aza-peptidomimetic analogs as potential HCV NS3-4A protease inhibitors
Peggy P. Huang, John T. Randolph, Charles A. Flentge, Larry L. Klein, Kevin Kurtz, Alex Konstantinidis, Warren M. Kati, Xiaolin Zhang, Vincent S. Stoll, Dale J. Kempf
Discovery of BMS-433771, a respiratory syncytial virus fusion inhibitor
Ny Sin, Kuo-Long Yu, Keith Combrink, Brian Venables, Xiangdong Alan Wang, Hatice Belgin Gulgeze, Rita L. Civiello, Kathleen F. Kadow, Christopher Cianci, Junius Clark, Eugene Genovese, Stacey Voss, Lucinda Lamb, Ivette Medina, Zheng Yang, Lisa Zadjura, Stella Huang, Dedong Wu, Qi Gao, Mark Krystal, Nicholas A. Meanwell
Inhibitors of respiratory syncytial virus fusion: Optimization of the C-5 subsituent
Xiangdong Alan Wang, Kuo-Long Yu, Kathleen F. Kadow, Christopher Cianci, Julia Roach, Mark Krystal, David R. Langley, Nicholas A. Meanwell
Isatin oximes as inhibitors of respiratory syncytial virus fusion
Brian L. Venables, Kuo-Long Yu, Bradley C. Pearce, Yi Zhang, Keith Combrink, Jan Thuring, Xiangdong Alan Wang, Rita L. Civiello, Hatice Belgin Gulgeze, Eugene Genovese, Christopher Cianci, Kathleen F. Kadow, Stacey Voss, Lucinda Lamb, Ivette Medina, Junius M. Clark, Zheng Yang, Lisa Zadjura, Stella Huang, Mark Krystal, Nicholas A. Meanwell
Discovery of TAK-242, a novel inhibitor of TLR4-mediated cytokine production as an anti-sepsis agent
Takashi Ichikawa, Masami Yamada, Masayuki Ii, Toru Yamano, Norikazu Tamura, Katsumi Itoh, Tomoyuki Kitazaki
New and improved 5,10-dihydrobenzo[b][1,8]napthyridine-N-oxides as the next generation NNRTI’s with better activity profiles against clinically relevant HIV-1 mutants
Anurag S Srivastava, Christine M. Tarby, Barry M. Johnson, Bhakthavatchalam Rajagopal, Matthew Curry, Qiyan Lin, Haisheng Wang, Anthony J. Cocuzza, Donna M. Bilder, Robert J. McHugh, Mona Patel, Lee T. Bacheler, Sharon Diamond, Susan Jeffrey, Ronald M. Klabe, Beverly C. Cordova, Sena Garber, Kelly Logue, Susan Erickson-Viitanen, George L. Trainor, James D. Rodgers
Linear-response study on the binding affinity of non-nucleoside RT inhibitors with HIV-1 reverse transcriptase
Guangyu Sun, Marc C Nicklaus
Discovery and synthesis of HIV integrase inhibitors: Dihydroxypyrimidine-4-carboxamides as novel potent and selective agents
Paola Pace, M. Emilia Di Francesco, Odalys Gonzalez Paz, Daria J. Hazuda, Ralph Laufer, Emanuela Nizi, Alessia Petrocchi, Michael Rowley, W.A. Schleif, Kara A. Stillmock, Marc V. Witmer, Vincenzo Summa
Discovery and synthesis of HIV integrase inhibitors: Development of potent bioavailable N-methyl pyrimidones
Cristina Gardelli, Emanuela Nizi, Marco Poma, Benedetta Crescenzi, Ester Muraglia, Paola Pace, Rita Scarpelli, Vincenzo Summa, Michael Rowley, Odalys Gonzalez Paz, Ralph Laufer, William A. Schleif, Kara A. Stillmock, Marc Witmer, Daria Hazuda
From dihydroxypyrimidine carboxylic acids to carboxamide HIV integrase inhibitors
Alessia Petrocchi, Paola Pace, Daria J. Hazuda, William A. Schleif, Kara A. Stillmock, Marc V. Witmer, Victor G. Matassa, Vincenzo Summa
HIV-1 integrase inhibitory peptides: Cyclization, dimerization, tetramerization and peptide inhibitory potency
Krzysztof Krajewski, Christophe Marchand, Yves Pommier, Peter P. Roller
Versatile synthesis of 2, 5A-Tat antisense chimeras for anti-HIV/AIDS
Longhu Zhou, Edgar R. Civitello, Nidhi Gupta, Ross Molinaro, Robert H. Silverman, Paul F. Torrence
Sophorolipids: Microbial glycolipids with anti-HIV and sperm-immobilizing activities
Vishal Shah, Gustavo F. Doncel, Abul Azim, Theodoros Seyoum, Kristin Eaton, Irina Zalenskaya, Rena Hagver, Richard Gross
HIV protease inhibitors with potential for once-daily dosing and reduced side effects
David A. DeGoey, William J. Flosi, David J. Grampovnik, Charles A. Flentge, Larry L. Klein, Clinton M. Yeung, Tatyana Dekhtyar, Lynn Colletti, Jeffrey F. Waring, Rita Ciurlionis, Kennan C. Marsh, James M. Schmidt, Sue J. Swanson, Vincent Stoll, Mulugeta Mamo, Hongmei Mo, Warren M. Kati, Akhteruzzaman Molla, Dale J. Kempf
Understanding the monophosphorylation efficiency of nucleosides by deoxycytidine kinase (dCK) and their mechanism of anti-HIV activity by molecular modeling
Vikas Yadav, Yunho Jin, Chung K. Chu
Reductive cleavage of 1,2,4,5-tetraoxane antimalarials
Bogdan A Solaja, Natasa Terzic, Kirsten Smith, Dejan Opsenica, Philip L Smith, Wilbur K. Milhous
Comparison between antimalarial spiroadmantyl 1,2,4-trioxane and 1,2,4-trioxolane pairs: Important balance between chemical reactivity and steric enviroment of the peroxide bond
Xiaofang Wang, Yuxiang Dong, Sergio Wittlin, Jonathan L. Vennerstrom
Strategies for the optimization of antimalarial 1,2,4-trioxolanes: From hydrophobic prototype OZ03 to drug candidate OZ277
Yuxiang Dong, Jonathan L. Vennerstrom
Identification of novel antileishmanial compounds through in silico pharmacophore development and database searching
Dawn A. Delfín, Apurba K. Bhattacharjee, Karl A. Werbovetz
Paper Withdrawn
Investigation of ecFabI’s interaction with substrate and inhibitors, and predicting binding affinities of inhibitors using computational structural biology tools
Salma Banu Rafi, Polina Novichenok, Kolappan Subramaniapillai, Caroline Kisker, Carlos Simmerling, Peter Tonge
N-thiolated 2-oxazolidinones: A new and novel class of synthetic antibacterial agents for methicillin-resistant Staphylococcus aureus (MRSA)
Rajesh Kumar Mishra, Kevin D Revell, Cristina Coates, Edward Turos, Sonja Dickey, Daniel V. Lim
Antibiotic-conjugated polyacrylate nanoparticles: New opportunities for development of anti-MRSA agents
Yang Helen Wang, Edward Turos, Kerriann Robyn Greenhalgh, Suresh Kumar Reddy Guntireddygari, Sonja Dickey, Daniel V. Lim
Synthesis and antimicrobial properties of novel S-nitroso β-lactams
Maya Kostova, Balbina Plotkin, Monika Konaklieva
Photoactive analogues of farnesyl diphosphate for studying protein prenylation
Juhua Xu, Olivier Henry, Mark D. Distefano
Synthesis of novel bicyclic and tricyclic aldehydes for the preparation of 6-methylidene penem derivatives: A novel class of broad spectrum beta-lactamase inhibitors
Osvaldo dos Santos, Tarek S. Mansour, Aranapakam Venkatesan, Fuk-Wah Sum, Yansong Gu, Lijing Chen, Zhong Li, Frank Lin, Gulnaz Khafizoa, Takao Abe, Hideki Ushirogochi, Itsuk Yamamura, Toshio Kumagai
Combinatorial library synthesis and biological evaluation of sets of novel ß-lactamase inhibitors
Qin Sun, H. Mario Geysen
Penicillin bound nanoparticles: A promising new way to save old antibiotics
Suresh Kumar Reddy Guntireddygari, Praveen Ramaraju, Edward Turos, Sonja Dickey, Daniel V. Lim
Reviving the clinical efficacy of kanamycin-B: Design and synthesis of novel kanamycin analogs and studies of their antibacterial activity against aminoglycoside resistant bacteria
Ravi Rai, Cheng-Wei Tom Chang
Design and synthesis of novel aminoglycosides and their antibacterial studies against aminoglycoside resistant bacteria
Ravi Rai, Cheng-Wei Tom Chang
Isolation, characterization, and enhanced antibacterial activity of components from Lomatium californicum
Shen-Chieh Chou, Molly C. Everngam, John J. Beck
Synthesis, biological activity, and X-ray crystal structural analysis of diaryl ether inhibitors of malarial enoyl acyl carrier protein reductase: 2'- and 4'-Substituted triclosan derivatives
Joel S. Freundlich, John W. Anderson, Dimitri Sarantakis, Hong-Ming Shieh, Edinson Lucumi, Mack Kuo, Min Yu, Luchezar Karagyozov, Guy A. Schiehser, David P. Jacobus, William R. Jacobs Jr., David A. Fidock, James C. Sacchettini
Designing water soluble dendritic amphiphiles for microbiocidal applications
Andre A. Williams, Eko, W. Sugandhi, Richard, V. Macri, Richard D. Gandour, Joseph, O. Falkinham
Design, development and synthesis of curcumin bioconjugates and their antibacterial and antifungal activity
Satyendra Mishra, Upma Narain, Roli Mishra, Krishna Misra
Paper Withdrawn
Bis-indoloquinolines: New antiinfective agents with low cytotoxicity
Seth Y. Ablordeppey, Xue Y. Zhu, Melissa Jacob, Shabana I. Khan, Larry A. Walker
Design and synthesis of novel thieno[2,3-d]pyrimidine derivatives as potential anti-bacterial agents
D. Ashok, Satish Goud Puppali, Mallikarjun Goud Puppali
New scaffold for polyvalent designs of antimicrobial peptides
Zhigang Liu, Heather Deshazer, Chunhui Zhou
Targeting the rhl quorum sensing cascade in Pseudomonas aeruginosa: C4 library of autoinducer analogs
Geetanjali J Jog, Hiro-aki Suga
Biologically active bis-(hinokitiolato)copper(II) complexes
GM. Arvanitis, M.E. Berardini, C. A. Heyer, S.Y. Kim, Douglas M. Ho
Chalcogenoxanthylium photosensitizers for use in photodynamic therapy (PDT) and photodynamic purging of blood-borne viral and bacterial pathogens
David J Donnelly, Michael R. Detty, Scott L Gibson, Russell Hilf, Stephen J Wagner, Andrey Skripchenko
The development of photoactivated caged biocides
Robert G. Brinson, Sarah L Leonard, Paul B. Jones
Polymer nanostructures in drug delivery: Treatment and prevention of burn wound infections
Kerriann Robyn Greenhalgh, Edward Turos, Yang Helen Wang, G. Suresh Kumar Reddy, Sonja Dickey
Studying the interactions of toxic metals with protein tyrosine kinases
Yousef Ahmadibeni, Keykavous Parang, Millie White, Gongqin Sun
Studies on the relationship between the structural and electronic parameters of some imido- substituted 2-chloro-1,4-naphthoquinones and their biological activities
Serenella Linares, Vernon R. Morris, Oladapo Bakare
Design of C1 domain-containing isozyme-specific ligands guided by the bioassay of diacylglycerol lactone libraries
Dehui Duan, Christopher C. Lai, James A. Kelley, Nancy Lewin, Peter M Blumberg, Victor E. Marquez

Symposium Grid -- Division of Medicinal Chemistry -- Session Listing

The 230th ACS National Meeting, in Washington, DC, Aug 28-Sept 1, 2005