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具有抗细菌和真菌活性的小偶氮苯衍生物。

Small azobenzene derivatives active against bacteria and fungi.

机构信息

Department of Pharmacy, University of Salerno, via Giovanni Paolo II, 132, 84084 Fisciano (Salerno), Italy.

出版信息

Eur J Med Chem. 2013 Oct;68:178-84. doi: 10.1016/j.ejmech.2013.07.030. Epub 2013 Aug 11.

Abstract

ATP synthase and protein kinase (PKs) are prime targets for drug discovery in a variety of diseases. It is well known that numerous stilbenes are capable to interact and inhibit ATP synthase and PKs. This work focuses on a series of azobenzene based molecules having high structural similarity with antimicrobial stilbenes. An investigation was carried out analyzing the potential toxicity of a large set of molecules by means of computational analysis. A small selection of potential low toxic molecules have been therefore synthesized, characterized and finally microbiologically tested. The synthesized compounds show potent bactericidal activity against Gram+ and a fungus, and are capable of inhibiting biofilm formation. Finally, the compounds demonstrated a thermal stability that makes them potential candidates for incorporation in polymer matrix for application as biomedical devices and food packaging.

摘要

三磷酸腺苷合酶和蛋白激酶(PKs)是各种疾病药物发现的主要靶点。众所周知,许多芪类物质能够相互作用并抑制三磷酸腺苷合酶和 PKs。这项工作集中在一系列具有与抗菌芪类物质高度结构相似性的偶氮苯类分子上。通过计算分析,对一大组分子的潜在毒性进行了研究。因此,选择了一小部分具有低毒性的潜在分子进行合成、表征和最终的微生物测试。合成的化合物对革兰氏阳性菌和真菌表现出很强的杀菌活性,并能够抑制生物膜的形成。最后,这些化合物表现出热稳定性,这使它们有可能被纳入聚合物基质中,作为生物医学设备和食品包装的应用。

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