Optimization of diarylamines as non-nucleoside inhibitors of HIV-1 reverse transcriptase

J Ruiz-Caro, A Basavapathruni, JT Kim…

Index: Ruiz-Caro, Juliana; Basavapathruni, Aravind; Kim, Joseph T.; Bailey, Christopher M.; Wang, Ligong; Anderson, Karen S.; Hamilton, Andrew D.; Jorgensen, William L. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 3 p. 668 - 671

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Citation Number: 34

Abstract

Following computational analyses, potential non-nucleoside inhibitors of HIV-1 reverse transcriptase have been pursued through synthesis and assaying for anti-viral activity. The general class Het–NH–Ph–U has been considered, where Het is an aromatic heterocycle and U is an unsaturated, hydrophobic group. Results for compounds with Het= 2-thiazoyl and 2-pyrimidinyl are the focus of this report.