Department of Organic and Bioorganic Chemistry, Faculty of Pharmacy in Hradec Králové, Charles University, Akademika Heyrovského 1203, 500 05 Hradec Králové, Czech Republic.
Department of Organic and Bioorganic Chemistry, Faculty of Pharmacy in Hradec Králové, Charles University, Akademika Heyrovského 1203, 500 05 Hradec Králové, Czech Republic.
Eur J Pharm Sci. 2018 Mar 1;114:318-331. doi: 10.1016/j.ejps.2017.12.013. Epub 2017 Dec 23.
Tuberculosis (TB) represents one of the leading causes of morbidity and mortality worldwide. Development of new potential drugs is essential because of the existence of latent TB and expansion of drug-resistant TB forms (multidrug-resistant and extensively drug-resistant tuberculosis). Triclosan is a widely used broad-spectrum biocidal agent. It has been shown to inhibit InhA, an essential enoyl acyl carrier protein reductase, resulting in the lysis of Mycobacterium tuberculosis. Triclosan can be considered as a promising compound for the inhibition of InhA and suppression of mycobacterial growth, because this polychlorinated molecule doesn't require any activation and it is able to affect the function of InhA directly. This approach enables to circumvent resistance to isoniazid. The aim of this review is to describe current knowledge about triclosan and its analogues as potential antimycobacterial agents.
结核病(TB)是全球发病率和死亡率的主要原因之一。由于潜伏性 TB 和耐药性 TB 形式(耐多药和广泛耐药性结核病)的存在,开发新的潜在药物至关重要。三氯生是一种广泛使用的广谱生物杀灭剂。它已被证明可以抑制 InhA,一种必需的烯酰基辅酶 A 还原酶,导致结核分枝杆菌的裂解。三氯生可以被认为是一种有前途的抑制 InhA 和抑制分枝杆菌生长的化合物,因为这种多氯化分子不需要任何激活,并且能够直接影响 InhA 的功能。这种方法可以避免对异烟肼的耐药性。本综述的目的是描述三氯生及其类似物作为潜在抗分枝杆菌药物的最新知识。