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…

文献索引：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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被引用次数: 23

摘要

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 ...