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Looking for new targets: Simple coumarins as antibacterial agents

机译:寻找新目标:简单的香豆素作为抗菌剂

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The dramatic worldwide increase of dangerous infections by resistant and multi-resistant microbes makes the search of new molecules and new chemical entities an important topic in Medicinal Chemistry. As the ideal drug candidate has not been attained, an intensive search for new and innovative antimicrobials is still needed. A small series of 3- aminoitrocoumarins without substitutions or substituted by methyl or methoxy groups at different positions were synthesized and evaluated for their antibacterial and antifungal activities against clinical isolates of Staphylococcus aureus, Escherichia coli and Candida albicans strains. Some of these structurally simple molecules exhibited antibacterial activity. The preliminary SAR study showed that the antibacterial activity against E. coli and S. aureus was dependent on the kind and position of the substitution pattern at the coumarin moiety.
机译:全球耐药菌和多重耐药菌在危险感染方面的急剧增加,使得寻找新分子和新化学实体成为药物化学中的重要课题。由于尚未获得理想的候选药物,因此仍需要深入研究新的和创新的抗菌剂。合成了一系列在不同位置没有取代或被甲基或甲氧基取代的3-氨基/硝基香豆素,并评估了它们对金黄色葡萄球菌,大肠杆菌和白色念珠菌菌株的临床分离株的抗菌和抗真菌活性。这些结构简单的分子中的一些表现出抗菌活性。 SAR的初步研究表明,对大肠杆菌和金黄色葡萄球菌的抗菌活性取决于香豆素部分上取代模式的种类和位置。

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