Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors

…, JM Hoffman, PL Darke, JA Zugay-Murphy…

Index: Dorsey; McDonough; McDaniel; Levin; Newton; Hoffman; Darke; Zugay-Murphy; Emini; Schleif; Olsen; Stahlhut; Rutkowski; Kuo; Lin; Chen; Michelson; Holloway; Huff; Vacca Journal of Medicinal Chemistry, 2000 , vol. 43, # 18 p. 3386 - 3399

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Citation Number: 42

Abstract

Recent results from human clinical trials have established the critical role of HIV protease inhibitors in the treatment of acquired immune-deficiency syndrome (AIDS). However, the emergence of viral resistance, demanding treatment protocols, and adverse side effects have exposed the urgent need for a second generation of HIV protease inhibitors. The continued exploration of our hydroxylaminepentanamide (HAPA) transition-state isostere ...