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Design, synthesis, and biological activity of a novel series of 2,5-disubstituted furans/pyrroles as HIV-1 fusion inhibitors targeting gp41
Faculty
Pharmacy
Year:
2011
Type of Publication:
Article
Pages:
6895-6898
Authors:
Abo-Dya, Nader E, Katritzky, Alan R, Avan, Ilker, Ibrahim, Tarek S, Tala, Srinivasa R, Jiang, Shibo, Lu, Hong, Zou, Peng, Abdelmajeid, Abdelmotaal, Debnath, Asim K
DOI:
10.1016/j.bmcl.2011.08.081
Journal:
BIOORGANIC \& MEDICINAL CHEMISTRY LETTERS PERGAMON-ELSEVIER SCIENCE LTD
Volume:
21
Research Area:
Pharmacology \& Pharmacy; Chemistry
ISSN
ISI:000296423700052
Keywords :
HIV-1 fusion inhibitors, Gp41, Furans, Pyrroles, ELISA
Abstract:
Based on molecular docking analysis of earlier results, we designed a series of 2,5-disubstituted furans/pyrroles (5a-h) as HIV-1 entry inhibitors. Compounds were synthesized by Suzuki-Miyaura cross coupling, followed by a Knoevenagel condensation or Wittig reaction. Four of these compounds were found to be effective in inhibiting HIV-1 infection, with the best compounds being 5f and 5h, which exhibited significant inhibition on HIV-1(IIIB) infection at micromolar levels with low cytotoxicity. These compounds are also effective in blocking HIV-1 mediated cell-cell fusion and the gp41 six-helix bundle formation, suggesting that they are also HIV-1 fusion inhibitors targeting gp41 and have potential to be developed as a new class of anti-HIV-1 agents. (C) 2011 Elsevier Ltd. All rights reserved.
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