合成嵌噻唑-诺卡酮衍生物作为有效的抗菌剂。
Synthesis of Chimeric Thiazolo-Nootkatone Derivatives as Potent Antimicrobial Agents.
机构信息
Department of Chemistry and Physics, College of Science and Mathematics, Arkansas State University, 72467, Jonesboro, AR, USA.
Department of Biological Sciences, College of Science and Mathematics, Arkansas State University, 72467, Jonesboro, AR, USA.
出版信息
ChemMedChem. 2021 Sep 6;16(17):2628-2637. doi: 10.1002/cmdc.202100230. Epub 2021 Jun 9.
Abstract
Nootkatone, an approved insecticide, is a well-known natural product from grapefruit. A series of fused-thiazole derivatives of nootkatone have been synthesized, and these new compounds were tested against several strains of bacteria. Some of these compounds are found to be potent antimicrobial agents against Staphylococcus aureus and Enterococcus faecium with minimum inhibitory concentration (MIC) values as low as 1.56 μg/mL. The lead compound is bactericidal and very potent against S. aureus persisters. These compounds are nontoxic to human cancer cell lines at 10 μm concentration.
摘要
诺卡酮是一种已被批准的杀虫剂，是葡萄柚中的一种知名天然产物。我们合成了一系列诺卡酮的稠合噻唑衍生物，并对这些新化合物进行了针对多种细菌株的测试。其中一些化合物被发现对金黄色葡萄球菌和屎肠球菌具有很强的抗菌活性，最低抑菌浓度 (MIC) 值低至 1.56μg/mL。先导化合物对耐甲氧西林金黄色葡萄球菌 (MRSA) 具有杀菌作用和很强的活性。这些化合物在 10μm 浓度下对人癌细胞系没有毒性。
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