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Synthesis and Biological Evaluation of 4-(3-Hydroxy-benzofuran-2-yl)coumarins

机译:4-(3-羟基-苯并呋喃-2-基)香豆素的合成及生物评价

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摘要

Various 4-bromomethylcoumarins (1a-k) were reacted with methyl salicylate to yield 2-(2-oxo-2H-chromen-4-ylmethoxy)-benzoic acid methyl esters (2a-k). Formations of (3a-k) were achieved by using DBU under microwave irradiation. Structures of all the compounds were established on the basis of their spectral data. All the compounds were testedin vitrofor their antimicrobial activity and cell cytotoxicity. All the tested compounds (2b-k) and (3a-k) were shown to be better activity againstStaphylococcus aureusthan the standardCiprofloxacin. The compound (3k) (R = 6-OMe) was found to be more potent cytotoxic than the standard5-fluorouracil.
机译:使各种4-溴甲基香豆素(1a-k)与水杨酸甲酯反应,得到2-(2-氧代-2H-铬-4-基氧基甲氧基)-苯甲酸甲酯(2a-k)。 (3a-k)的形成是通过在微波辐射下使用DBU实现的。所有化合物的结构均基于其光谱数据确定。所有化合物均在体外进行了抗微生物活性和细胞毒性测试。所有测试的化合物(2b-k)和(3a-k)对金黄色葡萄球菌的活性均优于标准环丙沙星。发现化合物(3k)(R = 6-OMe)比标准5-氟尿嘧啶具有更强的细胞毒性。

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