Synthesis and antimycobacterial activity of novel 1,3-dimethylisocyanurate derivatives

Eur J Med Chem. 2012 Jul:53:300-7. doi: 10.1016/j.ejmech.2012.04.014. Epub 2012 Apr 27.

Abstract

A series of novel 1,3-dimethylisocyanurates has been synthesized as potential inhibitors of β-ketoacyl synthase in mycobacteria. Most of the 25 compounds described and tested for their activity against M. tuberculosis have a bacteriostatic effect, comparable and even higher that of first-line antituberculosis drugs. These compounds are nontoxic, species-specific, exhibiting no activity against other bacterial species.

MeSH terms

  • Amides / chemistry
  • Animals
  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Anti-Bacterial Agents / toxicity
  • Chemistry Techniques, Synthetic
  • Mice
  • Microbial Sensitivity Tests
  • Mycobacterium tuberculosis / drug effects
  • Rats
  • Structure-Activity Relationship
  • Sulfonic Acids / chemistry
  • Triazines / chemical synthesis*
  • Triazines / chemistry
  • Triazines / pharmacology*
  • Triazines / toxicity

Substances

  • Amides
  • Anti-Bacterial Agents
  • Sulfonic Acids
  • Triazines
  • isocyanuric acid