Newer thiazolopyrimidine-based sulfonamides clubbed with benzothiazole moiety: synthesis and biological evaluation

作者：Patel Navin B^*; Purohit Amit C; Rajani Dhanji

来源：Medicinal Chemistry Research, 2014, 23(11): 4789-4802.

DOI：10.1007/s00044-014-1052-7

• Thiazolopyrimidines
• Sulfonamides
• Antimicrobial activity
• Antitubercular activity

A new class of thiazolopyrimidine-based sulfonamides (5a-j) was synthesized from a parent compound 2-methoxy benzoic acid by multistep reaction in order to find new agents to fight against microbial infections. Substituted thiazolopyrimidines (3a-e) were prepared by cyclocondensation of substituted thiazolidinediones (2a-e) with urea in the presence of acid catalyst P2O5. Finally, desired compounds (5a-j) were synthesized from intermediates (4a-e) prepared from compounds (3a-e) by chlorosulfonation followed by condensation with corresponding benzothiazole moiety. The synthesized compounds were characterized by IR, H-1-NMR, C-13-NMR spectral data, and elemental analysis, and were evaluated for in vitro antimicrobial activity against certain bacterial and fungal strains using the broth microdilution method as well as antitubercular activity against H(37)Rv using Lowenstein-Jensen agar method.

• 出版日期2014-11