Molecular Formula | C10H12N4OS |
Molar Mass | 236.29 |
Density | 1.2752 (rough estimate) |
Melting Point | 225-230 °C |
Appearance | powder to crystal |
Color | White to Orange to Green |
pKa | 11.35±0.70(Predicted) |
Storage Condition | Room Temprature |
Refractive Index | 1.6440 (estimate) |
Physical and Chemical Properties | Light yellow crystal or crystalline powder. Decomposition at 225-230 °c. Soluble in hot alcohol, slightly soluble in cold alcohol, very slightly soluble in water, insoluble in chloroform, ether, soluble in potassium hydroxide ethanol solution. |
In vitro study | 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. |
In vivo study | The K m and V max 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. |
Hazard Symbols | Xn - Harmful![]() |
Risk Codes | 22 - Harmful if swallowed |
Safety Description | 36 - Wear suitable protective clothing. |
WGK Germany | 3 |
RTECS | AE3850000 |
HS Code | 29309090 |
Toxicity | LD50 s.c. in mice: 1-2 g/kg (Bavin) |
biological activity | Thiacetazone (Thioacetazone) is an antituberculous agent containing thiourea and an orally active antibiotic. Thiacetazone has antibacterial effect and can inhibit the growth of Mycobacterium tuberculosis H37Rv (Mycobacterium tuberculosis H37Rv) with MIC value of 0.1 μg/mL. |
target | MIC: 0.1 μg/mL ( Mycobacterium tuberculosis H37Rv ) |
use | this product can inhibit tuberculosis and leprosy, and change the morphology, particle disappearance and chromatin of the bacteria. It was first used to treat leprosy, and its effect is not as good as sulfones, but it has a good effect on tuberculosis leprosy. |
Production method | It is obtained by the reaction of p-acetaminobenzaldehyde and hydrazine thiocyanate in glacial acetic acid at 104 ℃. The yield of this method is 95%. |