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Further Insights into the Oxidative Pathway of Thiocarbonyl-Type Antitubercular Prodrugs: Ethionamide, Thioacetazone, and Isoxyl.

Chemical research in toxicology

de Freitas Paulo T, Duhayon C, de França Lopes LG, Silva Sousa EH, Chauvin R, Bernardes-Génisson V.
PMID: 34319702
Chem Res Toxicol. 2021 Aug 16;34(8):1879-1889. doi: 10.1021/acs.chemrestox.1c00164. Epub 2021 Jul 28.

A chemical activation study of the thiocarbonyl-type antitubercular prodrugs, ethionamide (ETH), thioacetazone (TAZ), and isoxyl (ISO), was performed. Biomimetic oxidation of ethionamide using H

Isoniazid and thioacetazone may exhibit antitubercular activity by binding directly with the active site of mycolic acid cyclopropane synthase: Hypothesis based on computational analysis.

Bioinformation

Banerjee D, Bhattacharyya R.
PMID: 23055630
Bioinformation. 2012;8(16):787-9. doi: 10.6026/97320630008787. Epub 2012 Aug 24.

Isoniazid and thioacetazone are the two important antitubercular drugs. In case of thioacetazone it is established that it inhibits mycolic acid cyclopropane synthase but the exact binding site accounting for such inhibition is presently unknown. In case of isoniazid...

Synthesis and evaluation of new fluorinated anti-tubercular compounds.

Iranian journal of pharmaceutical research : IJPR

Esfahanizadeh M, Omidi K, Kauffman J, Gudarzi A, Shahraki Zahedani S, Amidi S, Kobarfard F.
PMID: 24734062
Iran J Pharm Res. 2014;13(1):115-26.

Treatment of tuberculosis (TB) and the discovery of effective new anti-tubercular drugs are among the most urgent priorities in health organizations all over the world. In the present study, fluorinated analogs of some of the most important anti-TB agents...

Showing 1 to 3 of 3 entries