Antituberculosis agents, I: Synthesis and antituberculosis activity of 2-aryl-1,3,4-thiadiazole derivatives

Pharmazie. 2001 Aug;56(8):610-2.

Abstract

The design, synthesis and antituberculosis activity of a series of 2-aryl-5-methylthio-1,3,4-thiadiazoles (5a-b), ethyl alpha-(5-aryl)-1,3,4-thiadiazole-2-ylthio)acetates (8a-b) and related compounds are described. All of the compounds were tested against Mycobacterium tuberculosis strain H37Rv in comparison to rifampicin. Six compounds exhibited a very good activity (MIC < 6.25 micrograms/ml, % Inhibition = 100).

MeSH terms

  • Acetates / chemical synthesis*
  • Acetates / pharmacology
  • Antitubercular Agents / chemical synthesis*
  • Antitubercular Agents / pharmacology
  • Magnetic Resonance Spectroscopy
  • Microbial Sensitivity Tests
  • Mycobacterium tuberculosis / drug effects
  • Spectrophotometry, Infrared
  • Thiadiazoles / chemical synthesis*
  • Thiadiazoles / pharmacology

Substances

  • Acetates
  • Antitubercular Agents
  • Thiadiazoles