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合成及四种新蓖麻酸衍生 1--烷基甘油的生物评价。

Synthesis and Biological Evaluation of Four New Ricinoleic Acid-Derived 1--alkylglycerols.

机构信息

Univ Rennes, Ecole Nationale Supérieure de Chimie de Rennes, CNRS, ISCR-UMR 6226, F-35000 Rennes, France.

AGIR, EA 4294, UFR of Pharmacy, Jules Verne University of Picardie, 80037 Amiens, France.

出版信息

Mar Drugs. 2020 Feb 15;18(2):113. doi: 10.3390/md18020113.

Abstract

A series of novel substituted 1--alkylglycerols (AKGs) containing methoxy (), -difluoro (), azide () and hydroxy () group at 12 position in the alkyl chain were synthesized from commercially available ricinoleic acid (). The structures of these new synthesized AKGs were established by NMR experiments as well as from the HRMS and elementary analysis data. The antimicrobial activities of the studied AKGs - were evaluated, respectively, and all compounds exhibited antimicrobial activity to different extents alone and also when combined with some commonly used antibiotics (gentamicin, tetracycline, ciprofloxacin and ampicillin). AKG was viewed as a lead compound for this series as it exhibited significantly higher antimicrobial activity than compounds -.

摘要

一系列新型取代的 1-烷基甘油(AKG)被合成出来,其中烷基链的 12 位上分别含有甲氧基()、二氟()、叠氮基()和羟基()。这些新型 AKG 是由商业可得的蓖麻油酸()合成的。这些新合成的 AKG 的结构通过 NMR 实验以及高分辨率质谱(HRMS)和元素分析数据得到了确定。对所研究的 AKG-进行了抗菌活性评估,结果表明,所有化合物单独使用时以及与一些常用抗生素(庆大霉素、四环素、环丙沙星和氨苄西林)联合使用时,均具有不同程度的抗菌活性。AKG 被视为该系列的先导化合物,因为它表现出比化合物-更高的抗菌活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e1be/7073722/66cef40d36ba/marinedrugs-18-00113-g001.jpg

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