Pharmacophore and structure–activity relationships of integrase inhibition within a dual inhibitor scaffold of HIV reverse transcriptase and integrase

Z Wang, J Tang, CE Salomon, CD Dreis…

Index: Wang, Zhengqiang; Tang, Jing; Salomon, Christine E.; Dreis, Christine D.; Vince, Robert Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 12 p. 4202 - 4211

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Citation Number: 31

Abstract

Rational design of dually active inhibitors against human immunodeficiency virus (HIV) reverse transcriptase (RT) and integrase (IN) has proved viable with 1-[(2-hydroxyethoxy) methyl]-6-(phenylthio) thymine (HEPT) type of non-nucleoside RT inhibitors (NNRTIs). To establish the pharmacophore and study the structure–activity relationships (SAR) of integrase inhibition within a previously disclosed RT/IN dual inhibitor scaffold, new ...