1. Academic Validation
  2. 5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series

5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series

  • Bioorg Med Chem Lett. 2004 Jun 21;14(12):3173-6. doi: 10.1016/j.bmcl.2004.04.008.
Yanping He 1 Fener Chen Guangfu Sun Yueping Wang Erik De Clercq Jan Balzarini Christophe Pannecouque
Affiliations

Affiliation

  • 1 Department of Chemistry, Fudan University, Shanghai 200433, People's Republic of China.
Abstract

The introduction of a beta-carbonyl group to the C-2 side chain of S-DABO led to the finding of a series of novel potent anti-HIV agent. Some derivatives proved to be highly effective in inhibiting HIV-1 replication at nanomolar concentrations. Furthermore, the novel S-DABOs differ from the classical NNRTIs in that some compounds are active against both HIV-1 and HIV-2. They might interfere with another target or at least act on RT in a different way as compared to typical NNRTIs.

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