Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: New, wide-spectrum anti-HIV-1 agents active at (Sub)-nanomolar level

Dante Rotili, Domenico Tarantino, Marino Artico, Maxim B. Nawrozkij, Emmanuel Gonzalez-Ortega, Bonaventura Clotet, Alberta Samuele, José A. Esté, Giovanni Maga, Antonello Mai

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50 Citations (Scopus)

Abstract

Here, we describe a novel small series of non-nucleoside reverse transcriptase inhibitors (NNRTIs) that combine peculiar structural features of diarylpyrimidines (DAPYs) and dihydro-alkoxy-benzyl-oxopyrimidines (DABOs). These DAPY-DABO hybrids (1-4) showed a characteristic SAR profile and a nanomolar anti-HIV-1 activity at both enzymatic and cellular level. In particular, the two compounds 4d and 2d, with a (sub)nanomolar activity against wild-type and clinically relevant HIV-1 mutant strains, were selected as lead compounds for next optimization studies. © 2011 American Chemical Society.
Original languageEnglish
Pages (from-to)3091-3096
JournalJournal of Medicinal Chemistry
Volume54
Issue number8
DOIs
Publication statusPublished - 28 Apr 2011

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