2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1

…, GB Roberts, SA Short, K Weaver, RJ Ott…

Index: Chan; Hong; Hunter III; Orr; Cowan; Sherman; Sparks; Reitter; Andrews III; Hazen; St. Clair; Boone; Ferris; Creech; Roberts; Short; Weaver; Ott; Ren; Hopkins; Stuart; Stammers Journal of Medicinal Chemistry, 2001 , vol. 44, # 12 p. 1866 - 1882

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Citation Number: 84

Abstract

A series of 2-amino-5-arylthiobenzonitriles (1) was found to be active against HIV-1. Structural modifications led to the sulfoxides (2) and sulfones (3). The sulfoxides generally showed antiviral activity against HIV-1 similar to that of 1. The sulfones, however, were the most potent series of analogues, a number having activity against HIV-1 in the nanomolar range. Structural-activity relationship (SAR) studies suggested that a meta substituent, ...