Synthesis of novel prodrugs of N,N'-bis[4(amidino)phenyl]pentanediamide

ORGN 381

Nageswara R. Kode, kode_rao@msn.com and Tien L Huang, thuang@xula.edu. College of Pharmacy, Xavier University of Louisiana, 1 Drexel Drive, New Orleans, LA 70125
N,N'-bis[4(amidino)phenyl]pentanediamide 701 made earlier at our Laboratory showed excellent anti-microbial activity against Pneumocystis carinii and Trypanosoma brucei and is a promising lead compound. In the present work we report the design and synthesis of a series of novel prodrugs of 701 that are expected to have better oral bioavailability and can be biotransformed in to the active diamidine. The poster will focus on the synthesis of the amidoxime, carboxy esters and 1,2,4-oxadiazoles of 701 as potential prodrugs.