PDF(Pubmed)
Abstract：
A series of triclosan azo-adducts were synthesized to investigate their structure-activity relationship against Mycobacterium tuberculosis and non-tuberculous mycobacteria. The series\' most potent compound was four and sixteen times more active than triclosan and rifabutin against drug-resistant Mycobacterium abscessus, respectively, while being less cytotoxic to human macrophages than triclosan on day one. Additionally, one of the azo-adducts was twice as efficient against M. tuberculosis as triclosan and twice as effective against Mycobacterium marinum as isoniazid. Furthermore, the synthesized azo-adducts were equally effective against M. abscessus strains overexpressing InhA, suggesting that these compounds work through a distinct mechanism.
摘要：
合成了一系列三氯生偶氮加合物，以研究它们对结核分枝杆菌和非结核分枝杆菌的构效关系。该系列最有效的化合物对耐药脓肿分枝杆菌的活性比三氯生和利福布汀高4至16倍，分别,而在第一天对人类巨噬细胞的细胞毒性低于三氯生。此外,其中一种偶氮加合物对结核分枝杆菌的效力是三氯生的两倍，对金黄色分枝杆菌的效力是异烟肼的两倍。此外，合成的偶氮加合物对过度表达InhA的脓肿分枝杆菌菌株同样有效，这表明这些化合物通过不同的机制起作用。
