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

J Med Chem. 2011 Apr 28;54(8):3091-6. doi: 10.1021/jm101626c.

Dante Rotili ¹, 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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Affiliation

1 Istituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Università degli Studi di Roma La Sapienza, Roma, Italy.

PMID: 21438533 DOI: 10.1021/jm101626c

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.

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