title: Pyrazolo[1,5-a]pyridine-3-carboxamide hybrids: Design, synthesis and evaluation of anti-tubercular activity.
abstract: A series of pyrazolo[1,5-a]pyridine-3-carboxamide hybrids were designed and evaluated as novel anti-tubercular agents. The representative hybrid 7 exhibited promising in vitro activity against susceptive strain H37Rv and a panel of drug-resistant Mtb strains with MIC values of 0.006 μg/mL and ranged from 0.003 to 0.014 μg/mL, respectively. More importantly, the hybrid 7 also showed very low cytotoxicity, and could significantly reduce the mycobacterial burden in a mouse model infected with autoluminescent H37Ra strain, which may serve as a lead compound for further development of new anti-tubercular agents.
authors.affiliation: School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou, 510632, China; State Key Laboratory of Respiratory Diseases, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Science, #190, Kai Yuan Avenue, Guangzhou, 510530, China. Electronic address: luxy2016@jnu.edu.cn.
authors.forename: Xiaoyun
authors.initials: X
authors.lastname: Lu
authors.affiliation: State Key Laboratory of Respiratory Diseases, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Science, #190, Kai Yuan Avenue, Guangzhou, 510530, China; University of Chinese Academy of Sciences, #19 Yuquan Road, Beijing, 100049, China.
authors.forename: Jian
authors.initials: J
authors.lastname: Tang
authors.affiliation: State Key Laboratory of Respiratory Diseases, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Science, #190, Kai Yuan Avenue, Guangzhou, 510530, China; University of Chinese Academy of Sciences, #19 Yuquan Road, Beijing, 100049, China.
authors.forename: Shengyang
authors.initials: S
authors.lastname: Cui
authors.affiliation: Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL, 60612, United States.
authors.forename: Baojie
authors.initials: B
authors.lastname: Wan
authors.affiliation: Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL, 60612, United States.
authors.forename: Scott G
authors.initials: SG
authors.lastname: Franzblauc
authors.affiliation: State Key Laboratory of Respiratory Diseases, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Science, #190, Kai Yuan Avenue, Guangzhou, 510530, China.
authors.forename: Tianyu
authors.initials: T
authors.lastname: Zhang
authors.affiliation: Guangzhou Eggbio Co., Ltd, 3 Ju Quan Road, Science Park, Guangzhou, 510663, China.
authors.forename: Xiantao
authors.initials: X
authors.lastname: Zhang
authors.affiliation: School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou, 510632, China; State Key Laboratory of Respiratory Diseases, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Science, #190, Kai Yuan Avenue, Guangzhou, 510530, China.
authors.forename: Ke
authors.initials: K
authors.lastname: Ding
mesh_terms: D000818:Animals; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D016923:Cell Death / Q000187:drug effects; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D004352:Drug Resistance, Microbial; D051379:Mice; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D011725:Pyridines / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: D000995:Antitubercular Agents; D011725:Pyridines
keywords: Anti-tubercular; Hybrid; Mtb; Pyrazolo[1,5-a]pyridine-3-carboxamide