ethionamide

Ethionamide (2-ethylthioisonicotinamide) 是一种抗结核抗生素。

Ethionamide HCl is the salt form of Ethionamide, a second-line antitubercular agent that inhibits mycolic acid synthesis. Ethionamide is a nicotinamide derivative, with antibacterial activity, used to treat tuberculosis. Although the exact mechanism of action of ethionamide is unknown, it may inhibit the synthesis of mycolic acid, a saturated fatty acid found in the bacterial cell wall, thereby inhibiting bacterial cell wall synthesis. This eventually leads to bacterial cell wall disruption and cell lysis. Ethionamide may be bacteriostatic or bactericidal in action, depending on the concentration of the drug at the site of infection and the susceptibility of the organism involved. It binds with NAD+ to form an adduct.

BDM31343是一种结核分枝杆菌中EthR抑制剂，可增以纳摩尔效力增强乙硫异烟胺的抗菌活性，同时提高溶解度和代谢稳定性。

SMARt751 靶向转录调控因子VirS，抑制其DNA结合能力，并上调mymA操纵子的表达，激活Ethionamide，增强其抗菌活性。SMARt751 提高了Ethionamide对结核分枝杆菌M. tuberculosis的效力，逆转其耐药性。在小鼠模型中，SMARt751 提升了Ethionamide的抗菌效果，同时降低了其有效剂量。此外，SMARt751 具备穿透血脑屏障的能力。

Thiocarlide (isoxyl) is a thiourea derivative that was used in the 1960s to successfully treat tuberculosis (TB). It has considerable antimycobacterial activity in vitro and is effective against multi-drug resistant strains of Mycobacterium tuberculosis in the range of 1-10 µg ml. [1] [2] At concentrations of 10 µM, isoxyl inhibits the synthesis of M. bovis during six hours of exposure which is similar to isoniazid (INH) and ethionamide (ETH), two other predominant anti-tuberculosis drugs. Unlike INH and ETH, isoxyl also partially inhibits the synthesis of fatty acids. Isoxyl shows no acute toxicity against primary macrophage cell cultures as demonstrated by diminution of redox activity.[2]

BDM31369 is an activator of ethionamide.