Discovery of new chemical entities as potential leads against Mycobacterium tuberculosis

A series of biheterocyclic derivatives were synthesized and evaluated for their anti-tubercular activities. The representive 2,6-dimethylpyrazolo[5,1-b]thiazole 10a exhibited strong suppressing function against H37Ra strain with MIC value of 0.03μg/mL in vitro, and significantly reduced the bacterial burden in an autoluminescent H37Ra infected mouse model.