2-(Alkyl/Aryl)amino-6-benzylpyrimidin-4(3 H)-ones as inhibitors of wild-type and mutant HIV-1: Enantioselectivity studies

Dante Rotili, Alberta Samuele, Domenico Tarantino, Rino Ragno, Ira Musmuca, Flavio Ballante, Giorgia Botta, Ludovica Morera, Marco Pierini, Roberto Cirilli, Maxim B. Nawrozkij, Emmanuel Gonzalez, Bonaventura Clotet, Marino Artico, José A. Esté, Giovanni Maga, Antonello Mai

Research output: Contribution to journalArticleResearchpeer-review

27 Citations (Scopus)

Abstract

The single enantiomers of two pyrimidine-based HIV-1 non-nucleoside reverse transcriptase inhibitors, 1 (MC1501) and 2 (MC2082), were tested in both cellular and enzyme assays. In general, the R forms were more potent than their S counterparts and racemates and (R)-2 was more efficient than (R)-1 and the reference compounds, with some exceptions. Interestingly, (R)-2 displayed a faster binding to K103N RT with respect to WT RT, while (R)-1 showed the opposite behavior. © 2012 American Chemical Society.
Original languageEnglish
Pages (from-to)3558-3562
JournalJournal of Medicinal Chemistry
Volume55
Issue number7
DOIs
Publication statusPublished - 12 Apr 2012

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