Design and synthesis of HIV protease inhibitors. Variations of the carboxyterminus of the HIV protease inhibitor L-682,679

…, WM Sanders, SL Graham, JM Wiggins…

Index: DeSolms; Giuliani; Guare; Vacca; Sanders; Graham; Wiggins; Darke; Sigal; Zugay; Emini; Schleif; Quintero; Anderson; Huff Journal of Medicinal Chemistry, 1991 , vol. 34, # 9 p. 2852 - 2857

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Citation Number: 29

Abstract

A series of tetrapeptide analogues of 1 (L-682,679), in which the carboxy terminus has been shortened and modified, was prepared and their inhibitory activity measured against the HIV protease in a peptide cleavage assay. Selected examples were tested as inhibitors of virus spread in cell culture. Compound 12 was a 10-fold more potent enzyme inhibitor than 1 in vitro and 30-fold more potent in inhibiting the viral spread in cells.