4-(3-羟基-苯并呋喃-2-基)香豆素的合成及生物学评价

Puttaraju Boregowda, Shivashankar Kalegowda, V. Rasal, J. Eluru, Ebenezer Koyye
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引用次数: 8

摘要

不同的4-溴甲基香豆素(1a-k)与水杨酸甲酯反应得到2-(2-氧- 2h -铬-4-基甲氧基)苯甲酸甲酯(2a-k)。DBU在微波照射下形成(3a-k)。所有化合物的结构都是根据它们的光谱数据确定的。对所有化合物进行了体外抗菌活性和细胞毒性试验。所有被测试的化合物(2b-k)和(3a-k)对金黄色葡萄球菌的活性都比标准环丙沙星更好。发现化合物(3k) (R = 6-OMe)比标准的5-氟尿嘧啶具有更强的细胞毒性。
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Synthesis and Biological Evaluation of 4-(3-Hydroxy-benzofuran-2-yl)coumarins
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 tested in vitro for their antimicrobial activity and cell cytotoxicity. All the tested compounds (2b-k) and (3a-k) were shown to be better activity against Staphylococcus aureus than the standard Ciprofloxacin. The compound (3k) (R = 6-OMe) was found to be more potent cytotoxic than the standard 5-fluorouracil.
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