TY - JOUR
T1 - Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: New, wide-spectrum anti-HIV-1 agents active at (Sub)-nanomolar level
AU - Rotili, Dante
AU - Tarantino, Domenico
AU - Artico, Marino
AU - Nawrozkij, Maxim B.
AU - Gonzalez-Ortega, Emmanuel
AU - Clotet, Bonaventura
AU - Samuele, Alberta
AU - Esté, José A.
AU - Maga, Giovanni
AU - Mai, Antonello
PY - 2011/4/28
Y1 - 2011/4/28
N2 - 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.
AB - 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.
U2 - 10.1021/jm101626c
DO - 10.1021/jm101626c
M3 - Article
SN - 0022-2623
VL - 54
SP - 3091
EP - 3096
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
IS - 8
ER -
