Department of Pharmacology, Baylor College of Medicine, 1 Baylor Plaza, Houston, TX 77030, United States.
Bioorg Med Chem Lett. 2012 Oct 1;22(19):6229-32. doi: 10.1016/j.bmcl.2012.08.012. Epub 2012 Aug 10.
Bacterial resistance to β-lactam antibiotics caused by class B metallo-β-lactamases (MBL), especially for certain hospital-acquired, Gram-negative pathogens, poses a significant threat to public health. We report several 2-substituted 4,5-dihydrothiazole-4-carboxylic acids to be novel MBL inhibitors. Structure activity relationship (SAR) and molecular modeling studies were performed and implications for further inhibitor design are discussed.
某些医院获得性革兰氏阴性病原体对β-内酰胺类抗生素的耐药性是由 B 类金属β-内酰胺酶（MBL）引起的，这对公共健康构成了重大威胁。我们报告了几种 2-取代的 4,5-二氢噻唑-4-羧酸，它们是新型的 MBL 抑制剂。进行了结构活性关系（SAR）和分子建模研究，并讨论了对进一步抑制剂设计的影响。
