3-Benzyl-2H-1,3-benzoxazine-2,4(3H)-diones, a new group of antimycobacterial compounds against potentially pathogenic strains

Farmaco. 2003 Nov;58(11):1137-49. doi: 10.1016/j.farmac.2003.07.004.

Abstract

A series of derivatives of 3-benzyl-2H-benzoxazine-2,4(3H)-dione substituted in positions 6, 7 or 8 on the benzoxazine, and in positions 3 or 4 on the benzyl moiety was synthesized. The compounds were evaluated for in vitro antimycobacterial activity against Mycobacterium avium and two strains of Mycobacterium kansasii. The disadvantage of the compounds is in their low solubility in water. The antimycobacterial activity of N-benzylsalicylamides correlates with that of 3-benzyl-2H-1,3-benzoxazin-2,4(3H)-diones and depends on the partition coefficients and electronic indexes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Benzophenones / chemistry
  • Benzophenones / pharmacology*
  • Benzoxazoles / chemistry
  • Benzoxazoles / pharmacology
  • Microbial Sensitivity Tests / methods
  • Mycobacterium / drug effects*
  • Mycobacterium / growth & development

Substances

  • Anti-Bacterial Agents
  • Benzophenones
  • Benzoxazoles