Acta Pharmaceutica Sinica B (Dec 2012)

Synthesis and biological evaluation of 8-substituted berberine derivatives as novel anti-mycobacterial agents

  • Yanxiang Wang,
  • Haigen Fu,
  • Yinghong Li,
  • Jiandong Jiang,
  • Danqing Song

DOI
https://doi.org/10.1016/j.apsb.2012.10.008
Journal volume & issue
Vol. 2, no. 6
pp. 581 – 587

Abstract

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Tuberculosis (TB) is a disease which kills two million people every year and infects over one-third of the world′s population. Eighteen new 8-substituted berberine derivatives were synthesized and evaluated for their anti-mycobacterial activities against Mycobacterium tuberculosis (M. tuberculosis) strain H37Rv. Among these compounds, compound 6i was the most effective antitubercular agent with an MIC of 1.0 μg/mL. Most importantly, compound 6i also exhibited a potent effect against clinically isolated rifampicin- and isoniazid-resistant M. tuberculosis strains, suggesting a different mode of action from the current drugs. Therefore, it shows potential for the development of new anti-TB agents.

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