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Design, Synthesis, and Biological Evaluation of Pyrazolo[1,5-a]pyridine-3-carboxamides as Novel Antitubercular Agents.
Tang, Jian; Wang, Bangxing; Wu, Tian; Wan, Junting; Tu, Zhengchao; Njire, Moses; Wan, Baojie; Franzblauc, Scott G; Zhang, Tianyu; Lu, Xiaoyun; Ding, Ke.
Afiliação
  • Tang J; 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.
  • Wang B; State Key Laboratory of Respiratory Diseases, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Science , #190 Kai Yuan Avenue, Guangzhou 510530, China ; College of Life Science, Anhui University , 111 Jiulong Road, Hefei 230601, China.
  • Wu T; State Key Laboratory of Respiratory Diseases, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Science , #190 Kai Yuan Avenue, Guangzhou 510530, China.
  • Wan J; State Key Laboratory of Respiratory Diseases, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Science , #190 Kai Yuan Avenue, Guangzhou 510530, China.
  • Tu Z; State Key Laboratory of Respiratory Diseases, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Science , #190 Kai Yuan Avenue, Guangzhou 510530, China.
  • Njire M; 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.
  • Wan B; Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago , 833 South Wood Street, Chicago, Illinois 60612, United States.
  • Franzblauc SG; Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago , 833 South Wood Street, Chicago, Illinois 60612, United States.
  • Zhang T; State Key Laboratory of Respiratory Diseases, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Science , #190 Kai Yuan Avenue, Guangzhou 510530, China.
  • Lu X; State Key Laboratory of Respiratory Diseases, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Science , #190 Kai Yuan Avenue, Guangzhou 510530, China.
  • Ding K; State Key Laboratory of Respiratory Diseases, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Science , #190 Kai Yuan Avenue, Guangzhou 510530, China.
ACS Med Chem Lett ; 6(7): 814-8, 2015 Jul 09.
Article em En | MEDLINE | ID: mdl-26191372
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.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Ano de publicação: 2015 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Ano de publicação: 2015 Tipo de documento: Article