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

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Resum

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.
Idioma originalAnglès
Pàgines (de-a)3558-3562
RevistaJournal of Medicinal Chemistry
Volum55
Número7
DOIs
Estat de la publicacióPublicada - 12 d’abr. 2012

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