Antitubercular potential of some semisynthetic analogues of phytol

Bioorg Med Chem Lett. 2010 Jan 15;20(2):508-12. doi: 10.1016/j.bmcl.2009.11.107. Epub 2009 Nov 26.

Abstract

Phytol, a diterpene alcohol was modified to several semisynthetic analogues. Some of the modifications were done logically to enhance lipophilicity of the molecule. Analogues 14, 16 and 18 exhibited antitubercular activity (MIC 15.6-50microg/mL) better than phytol (100microg/mL). The most potent analogue 18 was evaluated for in vivo toxicity in Swiss albino mice and was well tolerated by the experimental animals up to 300mg/kg body weight as a single oral acute dose.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antitubercular Agents / chemical synthesis*
  • Antitubercular Agents / chemistry
  • Antitubercular Agents / toxicity
  • Mice
  • Microbial Sensitivity Tests
  • Mycobacterium tuberculosis / drug effects
  • Oximes / chemical synthesis*
  • Oximes / chemistry
  • Oximes / toxicity
  • Phytol / analogs & derivatives*
  • Phytol / chemical synthesis
  • Phytol / chemistry
  • Phytol / toxicity

Substances

  • Antitubercular Agents
  • Oximes
  • Phytol