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基于漆树酸支架的抗耐甲氧西林金黄色葡萄球菌(MRSA)药物的分子设计。

Molecular design of anti-MRSA agents based on the anacardic acid scaffold.

作者信息

Green Ivan R, Tocoli Felismino E, Lee Sang Hwa, Nihei Ken-Ichi, Kubo Isao

机构信息

Department of Chemistry, University of the Western Cape, Bellville 7530, South Africa.

出版信息

Bioorg Med Chem. 2007 Sep 15;15(18):6236-41. doi: 10.1016/j.bmc.2007.06.022. Epub 2007 Jun 14.

DOI:10.1016/j.bmc.2007.06.022
PMID:17601740
Abstract

A series of anacardic acid analogues possessing different side chains viz. phenolic, branched, and alicyclic were synthesized and their antibacterial activity tested against methicillin-resistant Staphylococcus aureus (MRSA). The maximum activity against this bacterium occurred with the branched side-chain analogue, 6-(4',8'-dimethylnonyl)salicylic acid, and the alicyclic side-chain analogue, 6-cyclododecylmethyl salicylic acid, with the minimum inhibitory concentration (MIC) of 0.39 microg/mL, respectively. This activity was superior to that of the most potent antibacterial anacardic acid isolated from the cashew Anacardium occidentale (Anacardiaceae), apple and nut, that is, the 6-[8'(Z),11'(Z),14'-pentadecatrienyl]salicylic acid.

摘要

合成了一系列具有不同侧链(即酚类、支链和脂环族)的腰果酚酸类似物,并测试了它们对耐甲氧西林金黄色葡萄球菌(MRSA)的抗菌活性。对该细菌具有最大活性的是支链侧链类似物6-(4',8'-二甲基壬基)水杨酸和脂环族侧链类似物6-环十二烷基甲基水杨酸,其最低抑菌浓度(MIC)分别为0.39μg/mL。该活性优于从腰果(漆树科)、苹果和坚果中分离出的最有效的抗菌腰果酚酸,即6-[8'(Z),11'(Z),14'-十五碳三烯基]水杨酸。

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