SYNTHESIS AND BIOLOGICAL EVALUATION OF SUBSTITUTED THIAZOLAMINES, IMIDAZO [2,1b] THIAZOL-6-(5H)-ONES, THIAZOLO [3,2-a] PYRIMIDIN-5-ONES AND THIAZOLYL THIOUREAS

摘要

Substituted phenyl thiazole-2-amines (TA_(1-4)) when refluxed with ethyl acetoacetate using phosphorous oxychloride and poly phosphoric acid as a catalyst yielded thiazolo-pyrimidines (TP_(1-4)) and with chloroacetic acid in ethanol furnished imidazol-thiazoles (IT_(1-4)). Thiazolyl thioureas (TT_(1-4)) were synthesized by the reaction of TA_(1-4) with ammonium thiocynate in dilute hydrochloric acid. The structures of the synthesized compounds have been established on the basis of their spectral data and drug likeliness was analyzed using Molinspiration online resource. The in vitro tuberculostatic potential was evaluated against H_(37)Rv strain of Mycobacterium tuberculosis by REMA assay and showed moderate activity for compound IT2. Synthesized compounds were also screened against Staphylococcus aureus (MTCC 3160), Bacillus subtilis (MTCC 441), Escherichia coli (MTCC 40) and Pseudomonus aeruginosa (MTC 424) bacteria and showed significant activity.