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Tang J, Wang B, Wu T, et al. Design, Synthesis, and Biological Evaluation of Pyrazolo[1,5-a]pyridine-3-carboxamides as Novel Antitubercular Agents. ACS Med Chem Lett. 2015;6(7):814-8doi: 10.1021/acsmedchemlett.5b00176.
Tang, J., Wang, B., Wu, T., Wan, J., Tu, Z., Njire, M., Wan, B., Franzblauc, S. G., Zhang, T., Lu, X., & Ding, K. (2015). Design, Synthesis, and Biological Evaluation of Pyrazolo[1,5-a]pyridine-3-carboxamides as Novel Antitubercular Agents. ACS medicinal chemistry letters, 6(7), 814-8. https://doi.org/10.1021/acsmedchemlett.5b00176
Tang, Jian, et al. "Design, Synthesis, and Biological Evaluation of Pyrazolo[1,5-a]pyridine-3-carboxamides as Novel Antitubercular Agents." ACS medicinal chemistry letters vol. 6,7 (2015): 814-8. doi: https://doi.org/10.1021/acsmedchemlett.5b00176
Tang J, Wang B, Wu T, Wan J, Tu Z, Njire M, Wan B, Franzblauc SG, Zhang T, Lu X, Ding K. Design, Synthesis, and Biological Evaluation of Pyrazolo[1,5-a]pyridine-3-carboxamides as Novel Antitubercular Agents. ACS Med Chem Lett. 2015 Jun 11;6(7):814-8. doi: 10.1021/acsmedchemlett.5b00176. eCollection 2015 Jul 09. PMID: 26191372; PMCID: PMC4499832.
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ACS Med Chem Lett. 2015 Jun 11;6(7):814-8. doi: 10.1021/acsmedchemlett.5b00176. eCollection 2015 Jul 09.

Design, Synthesis, and Biological Evaluation of Pyrazolo[1,5-a]pyridine-3-carboxamides as Novel Antitubercular Agents.

ACS medicinal chemistry letters

Jian Tang, Bangxing Wang, Tian Wu, Junting Wan, Zhengchao Tu, Moses Njire, Baojie Wan, Scott G Franzblauc, Tianyu Zhang, Xiaoyun Lu, Ke Ding

Affiliations

  1. 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.
  2. 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.
  3. State Key Laboratory of Respiratory Diseases, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Science , #190 Kai Yuan Avenue, Guangzhou 510530, China.
  4. Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago , 833 South Wood Street, Chicago, Illinois 60612, United States.

PMID: 26191372 PMCID: PMC4499832 DOI: 10.1021/acsmedchemlett.5b00176

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

References

  1. PLoS One. 2013 Apr 04;8(4):e60531 - PubMed
  2. Science. 2008 Nov 28;322(5906):1392-5 - PubMed
  3. Nat Rev Drug Discov. 2013 May;12(5):388-404 - PubMed
  4. FEMS Microbiol Lett. 2010 Jul 1;308(1):1-7 - PubMed
  5. ACS Med Chem Lett. 2011 Jun 9;2(6):466-470 - PubMed
  6. Science. 2013 Jan 11;339(6116):130 - PubMed
  7. J Med Chem. 2001 Aug 16;44(17):2691-4 - PubMed
  8. PLoS One. 2012;7(12):e52951 - PubMed
  9. PLoS One. 2012;7(1):e29774 - PubMed
  10. Chem Pharm Bull (Tokyo). 1986 Jul;34(7):2828-32 - PubMed
  11. J Med Chem. 2014 Jun 26;57(12):5293-305 - PubMed
  12. Lancet Infect Dis. 2014 Apr;14(4):327-40 - PubMed
  13. J Clin Microbiol. 2014 Jan;52(1):291-7 - PubMed
  14. Jpn J Pharmacol. 1983 Apr;33(2):267-78 - PubMed
  15. ACS Med Chem Lett. 2013 Jul 11;4(7):675-679 - PubMed
  16. Science. 2005 Jan 14;307(5707):223-7 - PubMed
  17. Nature. 2000 Jun 22;405(6789):962-6 - PubMed
  18. Antimicrob Agents Chemother. 1997 May;41(5):1004-9 - PubMed
  19. N Engl J Med. 2014 Aug 21;371(8):723-32 - PubMed
  20. Nat Med. 2013 Sep;19(9):1157-60 - PubMed
  21. PLoS One. 2015 Mar 11;10(3):e0119341 - PubMed

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