6-Benzoyl-3-hydroxypyrimidine-2, 4-diones as dual inhibitors of HIV reverse transcriptase and integrase

J Tang, K Maddali, CD Dreis, YY Sham, R Vince…

Index: Tang, Jing; Maddali, Kasthuraiah; Dreis, Christine D.; Sham, Yuk Y.; Vince, Robert; Pommier, Yves; Wang, Zhengqiang Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 8 p. 2400 - 2402

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Citation Number: 23

Abstract

N-3-Hydroxylation of pyrimidine-2, 4-diones was recently found to yield inhibitors of both HIV- 1 reverse transcriptase (RT) and integrase (IN). An extended series of analogues featuring a benzoyl group at the C-6 position of the pyrimidine ring was synthesized. Through biochemical studies it was found that these new analogues are dually active against both RT and IN in low micromolar range. Antiviral assays confirmed that these new inhibitors are ...