Organic Communications Articles

A series of new 6-bromobenzo[d]thiazol-2(3H)-one derived 1,2,3-triazole derivatives (3a-j) have been synthesized by 1,3-dipolar cycloaddition of 6-bromobenzo[d]thiazol-2(3H)-one (2) with propargyl bromide and different aryl azides in a copper catalyzed one-pot reaction. All the synthesized compounds (3a-j) were evaluated for their in vitro cytotoxic activity against two human cancer cell lines MCF-7 and HeLa. The results showed that these compounds showed good cytotoxicity against the tested cell lines as compared with that of standard drug Cisplatin. The antibacterial activity of the newly synthesized triazole derivatives (3a-j) were also studied against different bacteria. The activity results showed that majority of compounds showed good to moderate antibacterial activity compared with positive control drug Streptomycin.

A series of new sulfonamide derivatives, 9-(substitutedbenzenesulfonyl)-6-chloro-9H-purines 7(a-e) and carbamate derivatives, 6-chloro-purine-9-carboxylic acid substituted alkyl/arylester 9(a-d), have been synthesized through an intermediate, sodium salt of 6-chloro-9(H)-purine (6) which was prepared by the treatment of 6-chloro-9(H)-purine (4) with sodium hydride. Structures of the newly synthesized compounds were elucidated by IR, NMR ( 1H and 13C), mass spectra and elemental analysis. Antimicrobial activity against three bacterial strains and three fungal strains at two different concentrations, 100 and 200 µg/mL including MIC values was investigated. Bio-screening data disclosed that most of the sulfonamide derivatives, 7a, 7c and 7d, and one carbamate derivative 9a showed promising antimicrobial activity having MIC values in the range of 18.0-25.0 µg/mL.