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一些杂环查耳酮类似物的合成及单独和联合抗生素的抗菌活性。

Synthesis and antibacterial activity of some heterocyclic chalcone analogues alone and in combination with antibiotics.

机构信息

Department of Medicinal Chemistry, School of Pharmacy, University of Medicine and Pharmacy at Ho Chi Minh City, 41 Dinh Tien Hoang, Dist. 1, Ho Chi Minh City 70000, Vietnam.

出版信息

Molecules. 2012 Jun 1;17(6):6684-96. doi: 10.3390/molecules17066684.

Abstract

A series of simple heterocyclic chalcone analogues have been synthesized by Claisen Schmidt condensation reactions between substituted benzaldehydes and heteroaryl methyl ketones and evaluated for their antibacterial activity. The structures of the synthesized chalcones were established by IR and ¹H-NMR analysis. The biological data shows that compounds p₅, f₆ and t₅ had strong activities against both susceptible and resistant Staphylococcus aureus strains, but not activity against a vancomycin and methicillin resistant Staphylococcus aureus isolated from a human sample. The structure and activity relationships confirmed that compounds f₅, f₆ and t₅ are potential candidates for future drug discovery and development.

摘要

一系列简单的杂环查耳酮类似物已经通过取代苯甲醛和杂芳基甲基酮之间的 Claisen-Schmidt 缩合反应合成,并评估了它们的抗菌活性。通过 IR 和 ¹H-NMR 分析确定了所合成查耳酮的结构。生物数据表明,化合物 p₅、f₆和 t₅对敏感和耐药金黄色葡萄球菌菌株均具有很强的活性,但对从人类样本中分离出的耐万古霉素和耐甲氧西林的金黄色葡萄球菌没有活性。结构和活性关系证实,化合物 f₅、f₆和 t₅是未来药物发现和开发的潜在候选物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/66ab/6268422/2f83d1c33033/molecules-17-06684-g001.jpg

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