Optimized Synthesis of New Thiosemicarbazide Derivatives with Tuberculostatic Activity

Int J Mol Sci. 2021 Nov 9;22(22):12139. doi: 10.3390/ijms222212139.

Abstract

Original results are presented in the field of research that addresses the extension of the reaction of residue of acyl-thiosemicarbazide fixation on the structure of 5-nitrobenzimidazole by a sulphonic group. The aim of the study is the increase of new thiosemicarbazide derivatives' applicative potential in the field of biochemistry, with a wide range of medical applications. The newly obtained compounds were characterized by using elemental analysis and spectral analysis (FT-IR and 1H NMR). A study regarding the optimization of the chemical reactions was made. The performed in vitro biological tests confirmed the tuberculostatic activity of three newly obtained compounds against Mycobacterium tuberculosis.

Keywords: 2-mercapto-benzimidazole; heterocyclic thiosemicarbazides; sulfonic derivatives; tuberculostatic activity.

MeSH terms

  • Antitubercular Agents / chemical synthesis*
  • Antitubercular Agents / chemistry
  • Antitubercular Agents / pharmacology
  • Humans
  • Magnetic Resonance Spectroscopy
  • Microbial Sensitivity Tests
  • Mycobacterium tuberculosis / drug effects*
  • Mycobacterium tuberculosis / pathogenicity
  • Semicarbazides / chemical synthesis*
  • Semicarbazides / chemistry
  • Semicarbazides / pharmacology
  • Spectroscopy, Fourier Transform Infrared
  • Structure-Activity Relationship
  • Tuberculosis / drug therapy*
  • Tuberculosis / microbiology

Substances

  • Antitubercular Agents
  • Semicarbazides
  • thiosemicarbazide