title: Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
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.
authors: Istituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Università degli Studi di Roma La Sapienza, Roma, Italy.
authors: Dante
authors: D
authors: Rotili
authors: Domenico
authors: D
authors: Tarantino
authors: Marino
authors: M
authors: Artico
authors: Maxim B
authors: MB
authors: Nawrozkij
authors: Emmanuel
authors: E
authors: Gonzalez-Ortega
authors: Bonaventura
authors: B
authors: Clotet
authors: Alberta
authors: A
authors: Samuele
authors: José A
authors: JA
authors: Esté
authors: Giovanni
authors: G
authors: Maga
authors: Antonello
authors: A
authors: Mai
mesh_terms: D019380:Anti-HIV Agents / Q000737:chemistry / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects*; D011743:Pyrimidines / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D019380:Anti-HIV Agents; D011743:Pyrimidines