Design, Synthesis, and Biological Evaluation of Pyrazolo[1,5-a]pyridine-3-carboxamides as Novel Antitubercular Agents
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- 作者：Jian Tang ; Bangxing Wang ; Tian Wu ; Junting Wan ; Zhengchao Tu ; Moses Njire ; Baojie Wan ; Scott G. Franzblauc ; Tianyu Zhang ; Xiaoyun Lu ; Ke Ding
- 刊名：ACS Medicinal Chemistry Letters
- 出版年：2015
- 出版时间：July 9, 2015
- 年：2015
- 卷：6
- 期：7
- 页码：814-818
- 全文大小：263K
- ISSN：1948-5875
文摘
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.