5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.

doi:10.1021/jm800340w

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5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.

Journal of medicinal chemistry - 14 Aug 2008

Nawrozkij Maxim B, Rotili Dante, Tarantino Domenico, Botta Giorgia, Eremiychuk Alexandre S, Musmuca Ira, Ragno Rino, Samuele Alberta, Zanoli Samantha, Armand-Ugón Mercedes, Clotet-Codina Imma, Novakov Ivan A, Orlinson Boris S, Maga Giovanni, Esté José A, Artico Marino, Mai Antonello

Abstract excerpt

A series of dihydro-alkylthio-benzyl-oxopyrimidines (S-DABOs) bearing a 2-aryl-2-oxoethylsulfanyl chain at pyrimidine C2, an alkyl group at C5, and a 2,6-dichloro-, 2-chloro-6-fluoro-, and 2,6-difluoro-benzyl substitution at C6 (oxophenethyl- S-DABOs, 6-8) is here described. The new compounds showed low micromolar to low nanomolar (in one case subnanomolar) inhibitory activity against wt HIV-1. Against clinically...

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PMID: 18630898
DOI: 10.1021/jm800340w

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