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Antibacterial activity of 2-alkynoic fatty acids against multidrug-resistant bacteria

机译：2-炔基脂肪酸对耐多药细菌的抗菌活性

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摘要

The first study aimed at determining the structural characteristics needed to prepare antibacterial 2- alkynoic fatty acids (2-AFAs) was accomplished by synthesizing several 2-AFAs and other analogs in 18-76% overall yields. Among all the compounds tested, the 2-hexadecynoic acid (2-HDA) displayed the best overall antibacterial activity against Gram-positive Staphylococcus aureus (MIC = 15.6 μg/mL), Staphylococcus saprophyticus (MIC = 15.5 μg/mL), and Bacillus cereus (MIC = 31.3 μg/mL), as well as against the Gram-negative Klebsiella pneumoniae (7.8 μg/mL) and Pseudomonas aeruginosa (MIC = 125 μg/mL). In addition, 2-HDA displayed significant antibacterial activity against methicillin-resistant S. aureus (MRSA) ATCC 43300 (MIC = 15.6 μg/mL) and clinical isolates of MRSA (MIC = 3.9 μg/mL). No direct relationship was found between the antibacterial activity of 2-AFAs and their critical micelle concentration (CMC) suggesting that the antibacterial properties of these fatty acids are not mediated by micelle formation. It was demonstrated that the presence of a triple bond at C-2 and the carboxylic acid moiety in 2-AFAs are important for their antibacterial activity. 2-HDA has the potential to be further evaluated for use in antibacterial formulations.
机译：旨在确定制备抗菌性2-炔属脂肪酸（2-AFA）所​​需的结构特征的第一项研究是通过以18-76％的总产率合成几种2-AFA和其他类似物来完成的。在所有测试的化合物中，2-十六碳酸（2-HDA）对革兰氏阳性金黄色葡萄球菌（MIC = 15.6μg/ mL），腐生葡萄球菌（MIC = 15.5μg/ mL）和芽孢杆菌具有最佳的总体抗菌活性。蜡样菌（MIC = 31.3μg/ mL），以及革兰氏阴性肺炎克雷伯菌（7.8μg/ mL）和铜绿假单胞菌（MIC = 125μg/ mL）。此外，2-HDA对耐甲氧西林的金黄色葡萄球菌（MRSA）ATCC 43300（MIC = 15.6μg/ mL）和临床分离的MRSA（MIC = 3.9μg/ mL）表现出显着的抗菌活性。在2-AFA的抗菌活性与其临界胶束浓度（CMC）之间未发现直接关系，这表明这些脂肪酸的抗菌特性不受胶束形成的影响。已证明2-AFA中C-2和羧酸部分存在三键对于其抗菌活性很重要。 2-HDA有潜力进一步评估用于抗菌制剂中。

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