✦ LIBER ✦

Structure-based drug design of nonpeptidic P2 substituents for HIV-1 protease inhibitors

✍ Scribed by Vincent J. Kalish; John H. Tatlock; Jay F. Davies II; Stephen W. Kaldor; Bruce A. Dressman; Siegfried Reich; Mark Pino; Dzuy Nyugen; Krzysztof Appelt; Linda Musick; Bor-wen Wu

Publisher: Elsevier Science
Year: 1995
Tongue: English
Weight: 290 KB
Volume: 5
Category: Article
ISSN: 0960-894X
DOI: 10.1016/0960-894x(95)00103-z

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✦ Synopsis

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 incorporated into the hydroxyethyl amine series to produce the potent antiviral compound (LY309391/AG1310).

Early research provided evidence that the retrovirus designated as human immunodeficiency virus (HIV-1) was responsible for the debilitating disease known as acquired immunodeficiency syndrome (AIDS). 1

Tragically no cure or effective treatment is currently available and the number of reported cases of AIDS

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