Small-Molecule Suppression of 尾-Lactam Resistance in Multidrug-Resistant Gram-Negative Pathogens

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• 作者：Christopher M. Brackett ; Roberta J. Melander ; Il Hwan An ; Aparna Krishnamurthy ; Richele J. Thompson ; John Cavanagh ; Christian Melander
• 刊名：Journal of Medicinal Chemistry
• 出版年：2014
• 出版时间：September 11, 2014
• 年：2014
• 卷：57
• 期：17
• 页码：7450-7458
• 全文大小：347K
• ISSN：1520-4804

文摘

Recent efforts toward combating antibiotic resistance in bacteria have focused on Gram-positive bacteria; however, multidrug-resistant Gram-negative bacteria pose a significant risk to public health. An orthogonal approach to the development of new antibiotics is to develop adjuvant compounds that enhance the susceptibility of drug-resistant strains of bacteria to currently approved antibiotics. This paper describes the synthesis and biological activity of a library of aryl amide 2-aminoimidazoles based on a lead structure from an initial screen. A small molecule was identified from this library that is capable of lowering the minimum inhibitory concentration of 尾-lactam antibiotics by up to 64-fold.