Coates Cristina, Long Timothy E, Turos Edward, Dickey Sonja, Lim Daniel V
Department of Chemistry, University of South Florida, Tampa, FL 33620, USA.
Bioorg Med Chem. 2003 Jan 17;11(2):193-6. doi: 10.1016/s0968-0896(02)00383-8.
N-Methylthio beta-lactams represent a novel family of antibacterial agents for methicillin-resistant Staphylococcus aureus (MRSA). The structure-activity functions and mechanism of action of these compounds, although still largely undefined, differ dramatically from those of all previously reported beta-lactam antibiotics. Prior work has established that the N-alkylthio moiety is required for antibacterial activity, and that a variety of unsaturated groups can be tolerated at C(4) of the lactam ring. This report describes the effect that unsaturation within the C(4) substituent has on antibacterial activity of these interesting new N-thiolated beta-lactams.
N-甲硫基β-内酰胺是一类针对耐甲氧西林金黄色葡萄球菌（MRSA）的新型抗菌剂。这些化合物的构效功能和作用机制虽然在很大程度上仍不明确，但与此前报道的所有β-内酰胺抗生素有显著差异。先前的研究已证实，N-烷硫基部分是抗菌活性所必需的，并且在内酰胺环的C(4)位可以耐受多种不饱和基团。本报告描述了C(4)取代基内的不饱和度对这些有趣的新型N-硫醇化β-内酰胺抗菌活性的影响。
