SYNTHESIS AND EVALUATION OF ANTITUBERCULAR AND ANTI FUNGAL ACTIVITY OF SOME NOVEL 6-(4-SUBSTITUTED ARYL)-2-(3,5-DIMETHYL-1H-PYRAZOL-1-YL) IMIDAZO[2,1-B] [1,3,4] THIADIAZOLE DERIVATIVES

摘要

The 6-(4-substituted aryl)-2-(3,5-dimethyl-1 H -pyrazol-1-yl)imidazo[2,1- b ][1,3,4]thiadiazole (2a to f) were prepared by treating 2-amino-5-(3,5-dimethyl-H-pyrazole-1yl)-1,3,4-thiadiazole with appropriate α-haloaryl ketones. The reaction 2 with morpholine using formaldehyde, acetic acid in methanol yielded the corresponding 5- morpholin-4-ylmethyl derivatives (3a-e). While compound 2 also produces the 5- pyrrolidine-4-ylmethyl derivatives (4a-e) by reaction with pyrrolidine using formaldehyde, acetic acid in methanol. The 5- piperidin-4-ylmethyl derivatives (5a-e) were obtained by treating compound 2 with piperidine using formaldehyde, acetic acid in methanol. The structures of the newly synthesized compounds confirmed by IR, NMR and Mass spectra. All the compounds were screened for antitubercular and antifungal activity. Some of the compound displayed very good antitubercular and antifungal activity.