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新型 3-乙酰基-2,5-二取代-1,3,4-恶二唑啉的生物活性、脂溶性和细胞毒性。

Biological Activity, Lipophilicity and Cytotoxicity of Novel 3-Acetyl-2,5-disubstituted-1,3,4-oxadiazolines.

机构信息

Chair and Department of Organic Chemistry, Faculty of Pharmacy, Medical University of Lublin, 4A Chodźki Street, 20-093 Lublin, Poland.

Chair and Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Medical University of Lublin, 1 Chodźki Street, 20-093 Lublin, Poland.

出版信息

Int J Mol Sci. 2021 Dec 20;22(24):13669. doi: 10.3390/ijms222413669.

Abstract

Antibiotic resistance is now a global problem, and the lack of effective antimicrobial agents for the treatment of diseases caused by resistant microbes is increasing. The 3-acetyl-2,5-disubstituted-1,3,4-oxadiazolines presented in this article may provide a good starting point for the development of potential new effective antimicrobial agents useful in the treatment of bacterial and fungal infections. Particular attention is drawn to the 1,3,4-oxadiazole derivative marked with the number with 5-nitrofuran-2-yl substituent in its chemical structure. This substance showed a strong bactericidal effect, especially against spp., and no cytotoxicity to the L929 normal cell line.

摘要

抗生素耐药性现在是一个全球性问题,而缺乏有效治疗耐药微生物引起的疾病的抗菌药物的情况正在加剧。本文介绍的 3-乙酰基-2,5-二取代-1,3,4-恶二唑啉可能为开发用于治疗细菌和真菌感染的潜在新型有效抗菌药物提供了一个良好的起点。特别值得注意的是,化学结构中带有 5-硝基呋喃-2-基取代基的 1,3,4-恶二唑啉衍生物。该物质对 spp. 表现出很强的杀菌作用,而且对 L929 正常细胞系没有细胞毒性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6038/8704594/6f2477887f43/ijms-22-13669-sch001.jpg

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