Functionalized aliphatic P2/P2′ analogs of HIV-1 protease inhibitor DMP323

…, LT Bacheler, MM Rayner, S Erickson-Viitanen…

Index: Smallheer, Joanne M.; McHugh, Robert J.; Chang, Chong-Hwan; Kaltenbach III, Robert F.; Worley, Tabitha V.; Klabe, Ronald M.; Bacheler, Lee T.; Rayner, Marlene M.; Erickson-Viitanen, Susan; Seitz, Steven P. Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 11 p. 1365 - 1370

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Citation Number: 3

Abstract

A series of analogs of HIV protease inhibitor DMP323 containing functionalized aliphatic P2/P2′ groups was prepared and evaluated for HIV protease inhibition and antiviral activity in a cell-based assay. Asymmetric compounds with a 5-hydroxypentyl substituent at P2 and a benzylic substituent at P2′ showed increased potency over the corresponding symmetrically substituted analogs.