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Design, Synthesis, and Evaluation of Tetrahydropyrimidinones as an Example of a General Approach to Nonpeptide HIV Protease Inhibitors

โœ Scribed by De Lucca, George V.; Liang, Jing; Aldrich, Paul E.; Calabrese, Joe; Cordova, Beverly; Klabe, Ronald M.; Rayner, Marlene M.; Chang, Chong-Hwan

Book ID
115528143
Publisher
American Chemical Society
Year
1997
Tongue
English
Weight
558 KB
Volume
40
Category
Article
ISSN
0022-2623

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The cyclizatlon of the linear hydroxyethylene isostere based HIV-PR inhibitors gave the delta lactam XQ921, which was found to have a K i = 9.4 uM. It is proposed that a major reason for the weaker potency of the lactam XQ921 compared to cycliv urea based inhibitors is the lack of a PI' substituent