Biaryl acids: novel non-nucleoside inhibitors of HIV reverse transcriptase types 1 and 2

J Milton, MJ Slater, AJ Bird, D Spinks, G Scott…

Index: Milton; Slater; Bird; Spinks; Scott; Price; Downing; Green; Madar; Bethell; Stammers Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 19 p. 2623 - 2628

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Citation Number: 39

Abstract

A series of biaryl acids has been found to show micromolar inhibition of the HIV reverse transcriptase (RT) from types 1 and 2 with IC50s in the micromolar range. The series was discovered by consideration of the polymerase active site and sub-structure searching of the company compound collection. Synthesis of analogues to investigate the SAR is described. Two of these compounds have shown inhibition of HIV-2 RT only.