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skos:definition |
MSH: A thiosemicarbazone that is used in association with other antimycobacterial agents in the initial and continuation phases of antituberculosis regimens. Thiacetazone containing regimens are less effective than the short-course regimen recommended by the International Union Against Tuberculosis and are used in some developing countries to reduce drug costs. (From Martindale, The Extra Pharmacopoeia, 30th ed, p217),NCI: A thiosemicarbazone prodrug with antitubercular activity. Although the exact mechanism by which thioacetazone exerts its effect has yet to be fully elucidated, this agent, upon activation by bacterial monooxygenase EtaA, appears to target and inhibit cyclopropane mycolic acid synthases (CMASs), a family of S-adenosyl-methionine-dependent methyl transferases responsible for cyclopropanation of mycolic acid. By inhibiting mycolic acid synthesis, the bacterial cell wall becomes more permeable and less resistant to injury which eventually leads to cell lysis. Mycolic acids, long-chain fatty aci
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