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[Et3NH][HSO4]-mediated efficient synthesis of novel xanthene derivatives and their biological evaluation
Journal of Saudi Chemical Society ( IF 5.8 ) Pub Date : 2020-03-30 , DOI: 10.1016/j.jscs.2020.03.006
Mashooq A. Bhat , Mohamed A. Al-Omar , Ahmed M. Naglah , Azmat Ali Khan

A series of novel 2-chloro quinoline incorporated xanthene derivatives were synthesized by using various 2-chloro 3-formyl quinoline, dimedone and triethylammonium hydrogen sulfate [Et3NH][HSO4] as a catalyst as well solvent to give good to excellent yields. All the xanthene compounds were investigated for their in vitro antimycobacterial activity against M. tuberculosis H37Ra (MTB) and M. bovis BCG strains. Among the synthesized compounds 3a, 3c, 3d, 3e, 3g, 3h and 3k were highly potent against both the strains. Most of the active compounds were non-cytotoxic against THP-1, HCT-116, A549 and MCF-7 cell lines. Most active compounds were having higher selectively index which suggested that these compound were highly potent.



中文翻译:

[Et 3 NH] [HSO 4 ]介导的新型x吨衍生物的高效合成及其生物学评价

以各种2-氯3-甲酰基喹啉,二甲酮和硫酸三乙铵[Et 3 NH] [HSO 4 ]为溶剂,合成了一系列新型的2-氯喹啉并入的an吨衍生物。。研究了所有the吨化合物对结核分枝杆菌H37Ra(MTB)和牛分枝杆菌BCG菌株的体外分枝杆菌活性。在合成的化合物3a3c3d,3e,3g3h3k中对两种菌株都非常有效。大多数活性化合物对THP-1,HCT-116,A549和MCF-7细胞系无细胞毒性。大多数活性化合物具有较高的选择性指数,这表明这些化合物是高效的。

更新日期:2020-03-30
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