ORGN 492 |
| Dramatic advances in the treatment of HIV infection have not obviated the need for new antiretroviral agents, given the propensity of HIV to mutate and the expense (and inconvenience) of current therapies. In this endeavor, protease inhibitors remain an area of significant interest. Mass screening of our compound collection produced several non-peptidic, pyrone-based protease inhibitors that were further modified using protein crystallography and structure-based design. The resulting dihydropyrones were optimized for antiviral activity and pharmacokinetic properties to give several clinical candidates, one of which will be discussed. This presentation will focus on the SAR of the dihydropyrone inhibitors with special emphasis on improvements in antiviral potency as well as the synthetic chemistry challenges encountered. |
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Technical Achievements in Organic Chemistry Awards
9:30 AM-12:00 PM, Wednesday, 31 August 2005 Washington DC Convention Center -- Ballroom C, Oral
Division of Organic Chemistry |