Design, Synthesis, and Biological Evaluation of Pyrazolo[1,5-a]pyridine-3-carboxamides as Novel Antitubercular Agents.
ACS Med Chem Lett, 2015/7/09;6(7):814-8.
Tang J[1], Wang B[2], Wu T[3], Wan J[3], Tu Z[3], Njire M[1], Wan B[4], Franzblauc SG[4], Zhang T[3], Lu X[3], Ding K[3]
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PMID: 26191372DOI: 10.1021/acsmedchemlett.5b00176
Impact factor: 4.632
Abstract
A series of pyrazolo[1,5-a]pyridine-3-carboxamide derivatives were designed and synthesized as new anti-Mycobacterium tuberculosis (Mtb) agents. The compounds exhibit promising in vitro potency with nanomolar MIC values against the drug susceptive H37Rv strain and a panel of clinically isolated multidrug-resistant Mtb (MDR-TB) strains. One of the representative compounds (5k) significantly reduces the bacterial burden in an autoluminescent H37Ra infected mouse model, suggesting its promising potential to be a lead compound for future antitubercular drug discovery.
Keywords: Antitubercular agent; H37Rv; pyrazolo[1,5-a]pyridine; structure−activity relationship; tuberculosis
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