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

Yanping He; Fener Chen; Guangfu Sun; Yueping Wang; Erik De Clercq; Jan Balzarini; Christophe Pannecouque

doi:10.1016/j.bmcl.2004.04.008

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.

Authors

Yanping He¹, Fener Chen, Guangfu Sun, Yueping Wang, Erik De Clercq, Jan Balzarini, Christophe Pannecouque

Affiliation

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

PMID: 15149669
DOI: 10.1016/j.bmcl.2004.04.008

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.

MeSH terms

Anti-HIV Agents / chemistry*
Anti-HIV Agents / pharmacology
Cell Line
HIV Reverse Transcriptase / antagonists & inhibitors*
HIV Reverse Transcriptase / metabolism
Humans
Pyrimidines / chemistry
Pyrimidines / pharmacology
Pyrimidinones / chemistry
Pyrimidinones / pharmacology
Reverse Transcriptase Inhibitors / chemistry*
Reverse Transcriptase Inhibitors / pharmacology

Substances

Anti-HIV Agents
DABO 546
Pyrimidines
Pyrimidinones
Reverse Transcriptase Inhibitors
HIV Reverse Transcriptase