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 TypeDr GradeEmail
Shibo JiangJiang, Shibo ResearcherDoctoratesjiang@nybloodcenter.org
Alan Roy KatritzkyKatritzky, Alan RoyResearcherDoctoratekatritzky@chem.ufl.edu

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