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Design, Synthesis, and Biological Activity of Novel 5-((Arylfuran/1H-pyrrol-2-yl)methylene)-2-thioxo-3-(3-(trifluoromethyl)p henyl)thiazolidin-4-ones as HIV-1 Fusion Inhibitors Targeting gp41
Faculty
Pharmacy
Year:
2011
Type of Publication:
Article
Pages:
572-579
Authors:
Abo-Dya, Nader E, Katritzky, Alan R, Avan, Ilker, Tala, Srinivasa R, Jiang, Shibo, Lu, Hong, Debnath, Asim K, Gyanda, Kapil, Lu, Lu
DOI:
10.1021/jm101014v
Journal:
JOURNAL OF MEDICINAL CHEMISTRY AMER CHEMICAL SOC
Volume:
54
Research Area:
Pharmacology \& Pharmacy
ISSN
ISI:000286306400013
Keywords :
Design, Synthesis, , Biological Activity , Novel 5-((Arylfuran/1H-pyrrol-2-yl)methylene)-2-thioxo-3-(3-(trifluoromethyl)p
Abstract:
On the basis of our earlier molecular docking analysis, we designed and synthesized 5-((arylfuran/1H-pyrrol-2-yl)methylene)-2-thioxo-3-(3-(trifluoromethyl)p henyl)thiazolidin-4-ones (12a-o) as HIV-1 entry inhibitors. Compounds 12a-o effectively inhibited infection by both laboratory-adapted and primary HIV-1 strains and blocked HIV-1 mediated cell cell fusion and gp41 six-helix bundle formation. Molecular docking analyses on two highly active inhibitors, 12b, containing a carboxylic acid group, and 12m, containing a tetrazole group, indicated that they both fit snugly into the hydrophobic cavity of HIV-1 gp41 from which each has important ionic interactions with lysine 574 (K574). By contrast, molecular docking of 12i, a less active compound containing a pyrrole instead of a furan ring, indicated a completely different orientation from 12b and 12m and missed critical interactions.
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