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.
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.
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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