4-烷基-4-噻吩并[2',3':4,5]吡咯并[2,3-]喹喔啉衍生物作为吲哚并[2,3-]喹喔啉的新型杂环类似物：合成与抗结核活性
4-Alkyl-4-thieno[2',3':4,5]pyrrolo[2,3-]quinoxaline Derivatives as New Heterocyclic Analogues of Indolo[2,3-]quinoxalines: Synthesis and Antitubercular Activity.
作者信息
Sadykhov Gusein A, Belyaev Danila V, Khramtsova Ekaterina E, Vakhrusheva Diana V, Krasnoborova Svetlana Yu, Dianov Dmitry V, Pervova Marina G, Rusinov Gennady L, Verbitskiy Egor V, Charushin Valery N
机构信息
Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences, S. Kovalevskoy Street, 22, Ekaterinburg 620137, Russia.
Department of Organic and Biomolecular Chemistry, Ural Federal University, Mira Street, 19, Ekaterinburg 620002, Russia.
出版信息
Int J Mol Sci. 2025 Jan 3;26(1):369. doi: 10.3390/ijms26010369.
The synthetic approach based on a sequence of Buchwald-Hartwig cross-coupling and annulation through intramolecular oxidative cyclodehydrogenation has been used for the construction of novel 4-alkyl-4-thieno[2',3':4,5]pyrrolo[2,3-]quinoxaline derivatives. For the first time, these polycyclic compounds were evaluated for antimycobacterial activity, including extensively drug-resistant strains. A reasonable bacteriostatic effect against HRv was demonstrated. A plausible mechanism for antimycobacterial activity of heterocyclic analogues of indolo[2,3-]quinoxalines has been advanced on the basis of their molecular docking data.
基于一系列布赫瓦尔德-哈特维希交叉偶联以及通过分子内氧化环脱氢进行环化反应的合成方法，已被用于构建新型4-烷基-4-噻吩并[2',3':4,5]吡咯并[2,3-]喹喔啉衍生物。首次对这些多环化合物进行了抗分枝杆菌活性评估，包括对广泛耐药菌株的评估。结果表明其对人耐药结核分枝杆菌具有合理的抑菌效果。基于吲哚并[2,3-]喹喔啉杂环类似物的分子对接数据，提出了一种关于其抗分枝杆菌活性的合理机制。
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