Discovery of new chemical entities as potential leads against Mycobacterium tuberculosis
Bioorganic & Medicinal Chemistry Letters(2016)
Abstract
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.
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Key words
Anti-tubercular agent,Imidazo[21-b]thiazole,Pyrazolo[51-b]thiazole,Scaffold hopping
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