A note to the biological activity of benzoxazine derivatives containing the thioxo group

Eur J Med Chem. 2010 Jul;45(7):2719-25. doi: 10.1016/j.ejmech.2010.02.037. Epub 2010 Feb 20.

Abstract

New 3-benzyl-4-thioxo-2H-1,3-benzoxazine-2(3H)-ones and 3-benzyl-2H-1,3-benzoxazine-2,4(3H)-dithiones were synthesized. The compounds were tested for in vitro antimycobacterial activity against Mycobacterium tuberculosis, Mycobacterium kansasii and Mycobacterium avium. The replacement of the carbonyl group by the thiocarbonyl group increased the antimycobacterial activity. The most active derivatives were more active than isonicotinhydrazide (INH). The cytotoxicity and the antiproliferative activity were studied as well.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemistry*
  • Anti-Bacterial Agents / pharmacology*
  • Benzoxazines / chemistry*
  • Benzoxazines / pharmacology*
  • Cell Proliferation / drug effects
  • HeLa Cells
  • Humans
  • Microbial Sensitivity Tests
  • Mycobacterium / drug effects

Substances

  • Anti-Bacterial Agents
  • Benzoxazines