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Design, synthesis and antiHIV activity of novel isatine-sulphonamides

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Author(s): Murugesh N | Chandramohan M | Debyser Z | Witvrouw M | Selvam P

Journal: Indian Journal of Pharmaceutical Sciences
ISSN 0250-474X

Volume: 70;
Issue: 6;
Start page: 779;
Date: 2008;
Original page

Keywords: Isatin | HIV-1 | MT-4 cells | HIV Integrase | sulphadimidine

ABSTRACT
A series of novel isatine-sulphonamide derivatives have been synthesized by combining isatin derivatives with sulphonamides. The structure of the synthesized compounds were elucidated by spectral analysis (IR, NMR and Mass). Investigation of anti-HIV activity was done against HIV-1(IIIB) in MT-4 cells and HIV integrase inhibitory activity. 4-(1-acetyl-5-methyl-2-oxoindolin-3-ylideneamino)-N-(4,6-dimethylpyrimidin-2-yl)benzenesulfonamide (SPIII-5ME-AC) inhibits the HIV Integrase enzymatic activity as both over all and strand transfer reaction and 4-(1-benzoyl-5-chloro-2-oxoindolin-3-ylideneamino)-N-(4,6-dimethylpyrimidin-2-yl)benzene sulfonamide (SPIII-5Cl-BZ) exhibits 36 percent maximum protection against HIV-1 at sub toxic concentration.
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