Synthesis Evaluation of Antitubercular Activity of Novel Mannich bases of imidazo 2,1-b1,3,4thiadiazoles

摘要

A series of 2-(4-methoxybenzyl)-6-aryl-5-pyrrolidin/piperidin/morpholin-1-ylmethylimidazo[ 2,1-b][1,3,4] thiadiazoles (3a-e, 4a-e & 5a-e) were synthesized by Mannich reaction by condensing 2-(4-methoxybenzyl)-6-arylimidazo[2,1-b][1,3,4]thiadiazoles with pyrrolidine, piperidine and morpholine. The title compounds were screened for antitubercular activity against Mycobacterium tuberculosis H_(37)Rv using the BACTEC 460 radiometric assay. Mannich bases with pyrrolidine substitution were found to be most active antitubercular agents. It proves that as the ring size decreases it becomes much potent in its activity. Pyrrolidine being 5 membered ring structure & further combined with imidazothiadiazole nucleus enhances the pharmacological activity.