Antituberculosis agents. V. Synthesis, evaluation of in vitro antituberculosis activity and cytotoxicity of some 2-(5-nitro-2-furyl)-1,3,4-thiadiazole derivatives

Farmaco. 2002 Sep;57(9):765-9. doi: 10.1016/s0014-827x(02)01277-6.

Abstract

A new series of 2-(5-nitro-2-furyl)-1,3,4-thiadiazole-2-sulfide, sulfoxide and sulfones were synthesized and evaluated for in vitro antituberculosis activity against Mycobacterium tuberculosis strain H37Rv using the radiometric BACTEC 460-TB methodology. Active compounds were also screened by serial dilution to assess toxicity to a VERO cell line. The results indicate that some compounds exhibited a good antituberculosis activity and the ethylthio analogue (5b) was the most active compound (MIC = 0.78 microg ml(-1)). Also, the cytotoxic effects indicate that compound 5b was the least toxic compound.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Antitubercular Agents / chemical synthesis*
  • Antitubercular Agents / pharmacology
  • Antitubercular Agents / toxicity
  • Cell Survival / drug effects
  • Chlorocebus aethiops
  • Inhibitory Concentration 50
  • Microbial Sensitivity Tests
  • Mycobacterium tuberculosis / drug effects*
  • Structure-Activity Relationship
  • Thiadiazoles / chemical synthesis*
  • Thiadiazoles / pharmacology
  • Thiadiazoles / toxicity
  • Vero Cells

Substances

  • Antitubercular Agents
  • Thiadiazoles