Inhibitors of the protease from human immunodeficiency virus: design and modeling of a compound containing a dihydroxyethylene isostere insert with high binding …

S Thaisrivongs, AG Tomasselli, JB Moon…

Index: Thaisrivongs, Suvit; Tomasselli, Alfredo G.; Moon, Joseph B.; Hui, John; McQuade, Thomas J.; et al. Journal of Medicinal Chemistry, 1991 ,  vol. 34,  # 8  p. 2344 - 2356

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Citation Number: 64

Abstract

The peptidomimetic template and the dihydroxyethylene isostere insert that were applied successfully to the design of renin inhibitors have been extended to the related protease from human immunodeficiency virus (HIV). The present report describes the structure-activity study leading to the identification of an inhibitor with a Ki of< 1 nM for the HIV type-1 protease (compound 11). This compound, containing a diol insert, is highly effective in ...