2. Academic Validation
  3. Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains

Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains

  • Bioorg Med Chem Lett. 2007 Apr 1;17(7):1956-60. doi: 10.1016/j.bmcl.2007.01.025.
Maria Letizia Barreca 1,  Angela Rao,  Laura De Luca,  Nunzio Iraci,  Anna-Maria Monforte,  Giovanni Maga,  Erik De Clercq,  Christophe Pannecouque,  Jan Balzarini,  Alba Chimirri
Affiliations

Affiliation

  • 1 Dipartimento Farmaco-Chimico, Università di Messina, Viale Annunziata, 98168 Messina, Italy. [email protected]
PMID: 17276064 DOI: 10.1016/j.bmcl.2007.01.025
Abstract

Molecular modeling studies led to the rational discovery of N(1)-arylsulfonyl-1,3-dihydro-2H-benzimidazol-2-one as a novel template for the design of new non-nucleoside Reverse Transcriptase inhibitors (NNRTIs) that are active against wild-type and mutant strains of HIV-1. It is worth noting that compound 3 proved to have antiretroviral activity similar to that of efavirenz and greater than that of nevirapine, two of the three NNRTIs currently available in antiretroviral therapy.

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