Amino Diol HIV Protease Inhibitors. 1. Design, Synthesis, and Preliminary SAR

…, E Gordon, M Alam, PF Lin, GS Bisacchi…

Index: Barrish, Joel C.; Gordon, Eric; Alam, Masud; Lin, Pin-Fang; Bisacchi, Gregory S.; et al. Journal of Medicinal Chemistry, 1994 , vol. 37, # 12 p. 1758 - 1768

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Citation Number: 65

Abstract

A series of HIV protease inhibitors containing a novel CZ symmetrical “aminodiol” core structure were prepared from amino acid starting materials. The ability of the aminodiols to inhibit HIV replication in cell culture is comparable to their ability to inhibit the isolated enzyme, a result compatible with good cell membrane penetration by this class of compounds. Optimization of the structure-activity in this series led to aminodiol9a (Ki= 100 ...