3-Hydroxypyrimidine-2, 4-diones as an inhibitor scaffold of HIV integrase

…, M Metifiot, YY Sham, R Vince, Y Pommier…

Index: Tang, Jing; Maddali, Kasthuraiah; Metifiot, Mathieu; Sham, Yuk Y.; Vince, Robert; Pommier, Yves; Wang, Zhengqiang Journal of Medicinal Chemistry, 2011 , vol. 54, # 7 p. 2282 - 2292

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Citation Number: 34

Abstract

Integrase (IN) represents a clinically validated target for the development of antivirals against human immunodeficiency virus (HIV). Inhibitors with a novel structure core are essential for combating resistance associated with known IN inhibitors (INIs). We have previously disclosed a novel dual inhibitor scaffold of HIV IN and reverse transcriptase (RT). Here we report the complete structure− activity relationship (SAR), molecular modeling, ...