title: Synthesis and anti-HIV activity of 4-[(1,2-dihydro-2-oxo-3H-indol-3-ylidene) amino]-N(4,6-dimethyl-2-pyrimidinyl)-benzene sulfonamide and its derivatives.
abstract: 4-[(1,2-Dihydro-2-oxo-3H-indol-3-ylidene) amino]-N(4,6-dimethyl-2-pyrimidinyl)-benzene sulphonamide and its derivatives were synthesized by reaction of isatin and its derivatives with sulphadimidine. Their chemical structures have been confirmed by IR, (1)H NMR data and elemental analysis. Investigation of anti-HIV activity of compounds were tested against replication of HIV-1 (IIIB) and HIV-2 (ROD) strains in acutely infected MT-4 cells and the activity compared with standard azidothymidine. Among the compounds tested, 4-[(1,2-dihydro-2 oxo-3H-indol-3-ylidene)amino]-N(4,6-dimethyl-2-pyrimidinyl)-benzene sulphonamide and its N-acetyl derivative were the most active compounds.
authors.affiliation: Bharat Ratna Kamarajar Liver Hospital and Research Centre, Madurai-625 001, Tamil Nadu, India. selvaamin@yahoo.co.in
authors.forename: P
authors.initials: P
authors.lastname: Selvam
authors.forename: M
authors.initials: M
authors.lastname: Chandramohan
authors.forename: E
authors.initials: E
authors.lastname: De Clercq
authors.forename: M
authors.initials: M
authors.lastname: Witvrouw
authors.forename: C
authors.initials: C
authors.lastname: Pannecouque
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002257:Carbonic Anhydrase Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D002460:Cell Line; D015497:HIV-1 / Q000187:drug effects; D015498:HIV-2 / Q000187:drug effects; D006801:Humans; D007510:Isatin / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology*; D013418:Sulfamethazine / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology*; D013449:Sulfonamides / Q000138:chemical synthesis / Q000494:pharmacology; D015215:Zidovudine / Q000737:chemistry / Q000494:pharmacology; D000096926:Benzenesulfonamides
chemical_list: D019380:Anti-HIV Agents; D002257:Carbonic Anhydrase Inhibitors; D007510:Isatin; D013418:Sulfamethazine; D013449:Sulfonamides; D015215:Zidovudine; D000096926:Benzenesulfonamides