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Design, synthesis and antiHIV activity of novel isatine-sulphonamides

Author(s): N Murugesh1, M Chandramohan2, Z Debyser3, M Witvrouw3, P Selvam4
1Institute of Pharmacology, Madurai Medical College, Madurai-625 020, India, 2Bharat Ratna Kamarajar Liver Hospital and Research Centre, Madurai-625 001, India, 3Molecular Medicine, Katholieke Universiteit Leuven and IRC KULAK, Leuven, Flanders, Belgium, 4 Arulmigu Kalasalingam College of Pharmacy, Anand nagar, Krishnankoil-626 190, India,

Correspondence Address:
P Selvam Arulmigu Kalasalingam College of Pharmacy, Anand nagar, Krishnankoil-626 190, India [email protected]

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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