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首页> 外文期刊>Chemistry: A European journal >Optimization and Mechanistic Studies of Psammaplin A Type Antibacterial Agents Active against Methicillin-Resistant Staphylococcus aureus (MRSA)
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Optimization and Mechanistic Studies of Psammaplin A Type Antibacterial Agents Active against Methicillin-Resistant Staphylococcus aureus (MRSA)

机译：抗甲氧西林金黄色葡萄球菌（MRSA）的Psammaplin A型抗菌剂的优化和机理研究

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摘要

As described in the preceding article, utilizing a novel combinatorial disulfide exchange strategy, a library of psammaplin A (1) analogues was constructed and screened for antibacterial activity leading to the identification of a collection of diverse lead compounds. These combinatorial leads were subsequently refined, through parallel synthesis, to afford a series of highly potent antibacterial agents (e.g. 17, 57, 58, 69, and 70), some possessing greater than 50-fold higher activities than the natural product. Evaluation of the selectivity and serum binding properties of some of the most promising compounds and preliminary studies directed at deciphering the mechanism of action of this novel class of antibacterial agents are also included.
机译：如前一篇文章所述，利用新颖的组合二硫键交换策略，构建了psammaplin A（1）类似物的文库，并筛选了其抗菌活性，从而鉴定了多种先导化合物。随后通过平行合成将这些组合的引线精制，以提供一系列高效的抗菌剂（例如17、57、58、69和70），其中一些具有比天然产物高50倍以上的活性。还包括对一些最有希望的化合物的选择性和血清结合特性的评估以及旨在破译这种新型抗菌剂作用机理的初步研究。

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