Structure-activity relationship of small-sized HIV protease inhibitors containing allophenylnorstatine

…, K Terashima, S Misawa, T Fukazawa…

Index: Mimoto, Tsutomu; Kato, Ryohei; Takaku, Haruo; Nojima, Satoshi; Terashima, Keisuke; Misawa, Satoru; Fukazawa, Tominaga; Ueno, Takamasa; Sato, Hideharu; Shintani, Makoto; Kiso, Yoshiaki; Hayashi, Hideya Journal of Medicinal Chemistry, 1999 , vol. 42, # 10 p. 1789 - 1802

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Citation Number: 92

Abstract

We designed and synthesized a new class of peptidomimetic human immunodeficiency virus (HIV) protease inhibitors containing a unique unnatural amino acid, allophenylnorstatine [Apns;(2 S, 3 S)-3-amino-2-hydroxy-4-phenylbutyric acid], with a hydroxymethylcarbonyl (HMC) isostere as the active moiety. A systematic evaluation of structure-activity relationships for HIV protease inhibition, anti-HIV activities, and ...