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[Antitubercular agents. 45. Antimycobacterial thiohydrazide].

K Waisser1, Z Odlerová, N Houngbedji

  • 1Lehrstuhl für anorganische und organische Chemie, Pharmazeutische Fakultät der Karls-Universität, Hradec Králové, DDR.

Zentralblatt Fur Mikrobiologie
|January 1, 1989
PubMed
Summary

This study explored thiohydrazides against tuberculosis and Mycobacterium kansasii. The compounds showed moderate activity, with higher concentrations needed for M. kansasii infections.

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Area of Science:

  • Medicinal Chemistry
  • Microbiology
  • Organic Synthesis

Context:

  • Tuberculosis remains a significant global health threat.
  • Drug-resistant strains of Mycobacterium tuberculosis necessitate novel therapeutic agents.
  • Mycobacterium kansasii presents a diagnostic challenge and can cause pulmonary disease.

Purpose:

  • To synthesize and evaluate the antimycobacterial activity of novel thiohydrazides.
  • To investigate the structure-activity relationships of these compounds.
  • To compare efficacy against Mycobacterium tuberculosis and Mycobacterium kansasii.

Summary:

  • Thiohydrazides incorporating an oxalic acid moiety were synthesized and tested.
  • All compounds exhibited moderate antimycobacterial activity.

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  • Minimal inhibitory concentrations were approximately three times higher for Mycobacterium kansasii compared to Mycobacterium tuberculosis.

    • Impact:

    • Identified a promising class of compounds for further antimycobacterial drug development.
    • Highlighted the potential of specific aromatic thiohydrazides with RM values between 2.2-2.6.
    • Provided insights into differential activity against key mycobacterial species.