酰基脯氨酰胺类：一类具有体内抗菌活性的新型肽脱甲酰酶抑制剂。
Acylprolinamides: a new class of peptide deformylase inhibitors with in vivo antibacterial activity.
机构信息
Infectious Diseases Center of Excellence for Drug Discovery, Antibacterial Discovery Performance Unit, GlaxoSmithKline, Collegeville, PA 19426, USA.
出版信息
Bioorg Med Chem Lett. 2012 Jun 15;22(12):4028-32. doi: 10.1016/j.bmcl.2012.04.086. Epub 2012 Apr 25.
PMID:22579486
Abstract
A new class of PDF inhibitor with potent, broad spectrum antibacterial activity is described. Optimization of blood stability and potency provided compounds with improved pharmacokinetics that were suitable for in vivo experiments. Compound 5c, which has robust antibacterial activity, demonstrated efficacy in two respiratory tract infection models.
摘要
本文描述了一类具有强大、广谱抗菌活性的新型 PDF 抑制剂。通过优化血液稳定性和效力，得到了具有改善的药代动力学特性的化合物，适合进行体内实验。具有强大抗菌活性的化合物 5c 在两种呼吸道感染模型中均显示出疗效。
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