Biological Activity
Thiacetazone (Thioacetazone) is a thiourea-containing antitubercular agent and is an orally active antibiotic. Thiacetazone has antibacterial action, which inhibits growth of Mycobacterium tuberculosis H37Rv with a MIC value of 0.1 μg/mL[1].
In Vitro
Thiacetazone is a prodrug that is activated by the mycobacterial monooxygenase EthA, which is also the activator of two other anti-tuberculosis agents, Ethionamide and Isoxyl[3].
In Vivo
The Km and Vmax values for the N-deacetylation of Thiacetazone are 0.57 mM and 0.123 nmol of p-aminobenzaldehydethiosemicarbazone formed/min/mg cytosolic protein, respectively. The ability to metabolize Thiacetazone is the same in the livers of cat, mouse and human, but lagged significantly in that of rat[2].
References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.