2. Academic Validation
  3. Design and synthesis of N₁-aryl-benzimidazoles 2-substituted as novel HIV-1 non-nucleoside reverse transcriptase inhibitors

Design and synthesis of N₁-aryl-benzimidazoles 2-substituted as novel HIV-1 non-nucleoside reverse transcriptase inhibitors

  • Bioorg Med Chem. 2014 Feb 15;22(4):1459-67. doi: 10.1016/j.bmc.2013.12.045.
Anna-Maria Monforte 1,  Stefania Ferro 2,  Laura De Luca 2,  Giuseppa Lo Surdo 2,  Francesca Morreale 2,  Christophe Pannecouque 3,  Jan Balzarini 3,  Alba Chimirri 2
Affiliations

Affiliations

  • 1 Dipartimento di Scienze del Farmaco e Prodotti per la Salute, Università di Messina, Viale Annunziata, I-98168 Messina, Italy. Electronic address: ammonforte@unime.it.
  • 2 Dipartimento di Scienze del Farmaco e Prodotti per la Salute, Università di Messina, Viale Annunziata, I-98168 Messina, Italy.
  • 3 Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium.
PMID: 24457088 DOI: 10.1016/j.bmc.2013.12.045
Abstract

A series of novel N1-aryl-2-arylthioacetamido-benzimidazoles were synthesized and evaluated as inhibitors of human immunodeficiency virus type-1 (HIV-1). Some of them proved to be effective in inhibiting HIV-1 replication at submicromolar and nanomolar concentration acting as HIV-1 non-nucleoside RT inhibitors (NNRTIs), with low cytotoxicity. The preliminary structure-activity relationship (SAR) of these new derivatives was discussed and rationalized by docking studies.

Keywords

HIV-1 reverse transcriptase; N(1)-Aryl-benzimidazoles 2-substituted; NNRTIs; Synthesis.

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