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

Jing Tang, Kasthuraiah Maddali, Christine D. Dreis, Yuk Y. Sham, Robert Vince, Yves Pommier, Zhengqiang Wang

Research output: Contribution to journalArticle

32 Scopus citations

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 active against HIV-1 in cell culture at nanomolar to low micromolar range, further validating 3-hydroxypyrimidine-2,4-diones as a viable scaffold for antiviral development.

Original languageEnglish (US)
Pages (from-to)2400-2402
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume21
Issue number8
DOIs
StatePublished - Apr 15 2011

Keywords

  • 6-Benzoyl-3-hydroxypyrimidine-2,4-diones
  • Dual inhibitors
  • HIV
  • Integrase
  • Reverse transcriptase

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