Inhibitors of human immunodeficiency virus type 1 protease containing 2-aminobenzyl-substituted 4-amino-3-hydroxy-5-phenylpentanoic acid: synthesis, activity, and …

P Lehr, A Billich, B Charpiot, P Ettmayer…

Index: Lehr; Billich; Charpiot; Ettmayer; Scholz; Rosenwirth; Gstach Journal of Medicinal Chemistry, 1996 , vol. 39, # 10 p. 2060 - 2067

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Citation Number: 36

Abstract

Systematic modifications of HIV protease inhibitor (2 R, 3 S, 4 S)-4-[[(benzyloxycarbonyl)-l- valyl] amino]-3-hydroxy-2-[(4-methoxybenzyl) amino]-5-(phenylpentanoyl)-l-valine 2- (aminomethyl) benzimidazole amide led to a novel series of inhibitors with a shortened, modified carboxy terminus. Their synthesis, in vitro enzyme inhibitory data, and antiviral activities are reported. Of particular interest are derivatives featuring the (1 S, 2 R)-1- ...