Alcaraz Matthéo, Seboletswe Pule, Manhas Neha, Kremer Laurent, Singh Parvesh, Kumar Vipan
Department of Chemistry, Guru Nanak Dev University, Amritsar, India.
Centre National de la Recherche Scientifique UMR 9004, Institut de Recherche en Infectiologie de Montpellier (IRIM), Université de Montpellier, 1919 route de Mende, 34293, Montpellier, France.
Heliyon. 2023 Nov 10;9(11):e22182. doi: 10.1016/j.heliyon.2023.e22182. eCollection 2023 Nov.
A series of triclosan azo-adducts were synthesized to investigate their structure-activity relationship against and non-tuberculous mycobacteria. The series' most potent compound was four and sixteen times more active than triclosan and rifabutin against drug-resistant , respectively, while being less cytotoxic to human macrophages than triclosan on day one. Additionally, one of the azo-adducts was twice as efficient against as triclosan and twice as effective against as isoniazid. Furthermore, the synthesized azo-adducts were equally effective against strains overexpressing InhA, suggesting that these compounds work through a distinct mechanism.
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。该系列中最有效的化合物对耐药结核分枝杆菌的活性分别比三氯生和利福布汀高4倍和16倍,且在第一天对人巨噬细胞的细胞毒性比三氯生小。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,对非结核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表达InhA的结核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。