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Document Details
Document Type
:
Article In Journal
Document Title
:
Design, synthesis, and biological activity of a novel series of 2,5-disubstituted furans/pyrroles as HIV-1 fusion inhibitors targeting gp41
Design, synthesis, and biological activity of a novel series of 2,5-disubstituted furans/pyrroles as HIV-1 fusion inhibitors targeting gp41
Subject
:
Chemistry
Document Language
:
English
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-1IIIB 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.
ISSN
:
0960-894X
Journal Name
:
Bioorganic and Medicinal Chemistry Letters
Volume
:
21
Issue Number
:
22
Publishing Year
:
1432 AH
2011 AD
Article Type
:
Article
Added Date
:
Wednesday, March 14, 2012
Researchers
Researcher Name (Arabic)
Researcher Name (English)
Researcher Type
Dr Grade
Email
Shibo Jiang
Jiang, Shibo
Researcher
Doctorate
sjiang@nybloodcenter.org
Alan Roy Katritzky
Katritzky, Alan Roy
Researcher
Doctorate
katritzky@chem.ufl.edu
Files
File Name
Type
Description
32647.pdf
pdf
Abstract
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