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新型具有抗抗生素耐药菌株活性的卡多醇类抗生素类似物。

New antibacterial cadiolide analogues active against antibiotic-resistant strains.

机构信息

Normandie Univ, CNRS, INSA Rouen, UNIROUEN, COBRA (UMR 6014 and FR 3038), 76000 Rouen, France; Laboratoire de Catalyse et Synthèse en Chimie Organique, Faculté des Sciences, Université Abou-Bekr Belkaid, BP 119, 13000 Tlemcen, Algeria.

Laboratoire de Microbiologie Signaux et Microenvironement (LMSM) EA 4312, Normandie Université, UNIROUEN, Evreux, France; Faculty of Health: Medicine, Dentistry and Human Sciences, University of Plymouth, Plymouth, United-Kingdom.

出版信息

Bioorg Med Chem Lett. 2020 Nov 1;30(21):127580. doi: 10.1016/j.bmcl.2020.127580. Epub 2020 Sep 25.

Abstract

The synthesis of new cadiolide analogues was carried out using a one-pot multi component synthesis. The antibacterial activity of these molecules was evaluated on standard and antibiotic resistant bacterial strains chosen for their involvement in human health or in food-born poisoning. Four molecules have shown good activities with MICs of 2 μg/mL. The introduction of an indole group or the conversion of the lactone into lactam have highlighted two new families of molecules with promising antibacterial activity. In addition, most of these active molecules are devoid of cytotoxic activity against keratinocyte cells.

摘要

采用一锅多组分合成法合成了新的卡多内酯类似物。根据其在人类健康或食源性中毒中的作用,选择标准和抗生素耐药的细菌菌株来评估这些分子的抗菌活性。四种分子表现出良好的活性,MIC 值为 2μg/mL。引入吲哚基团或内酯转化为内酰胺,突出了具有有前途的抗菌活性的两个新的分子家族。此外,这些活性分子大多对角质形成细胞无细胞毒性。

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