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Structure-Based Design of Novel HIV-1 Protease Inhibitors To Combat Drug Resistance

โœ Scribed by Ghosh, Arun K.; Sridhar, Perali Ramu; Leshchenko, Sofiya; Hussain, Azhar K.; Li, Jianfeng; Kovalevsky, Andrey Yu.; Walters, D. Eric; Wedekind, Joseph E.; Grum-Tokars, Valerie; Das, Debananda; Koh, Yasuhiro; Maeda, Kenji; Gatanaga, Hiroyuki; Weber, Irene T.; Mitsuya, Hiroaki


Book ID
120521188
Publisher
American Chemical Society
Year
2006
Tongue
English
Weight
398 KB
Volume
49
Category
Article
ISSN
0022-2623

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The cocrystal structures of LY289612 and LY297135 were used as a starting point in the design of nonpeptidic HIV-1 protease inhibitors. This report details the discovery of a series of novel aromatic P2 replacement groups. The 3-hydroxy-2-methyl benzoic acid group, discovered in AG1254, was incorpor