Department of Antibiotics and Microbiology, National Medicines Institute, Chełmska 30/34, 00-725 Warsaw, Poland.
Bioorg Med Chem. 2013 Feb 1;21(3):577-91. doi: 10.1016/j.bmc.2012.11.036. Epub 2012 Dec 5.
The oxazolidinones are a new and potent class of antimicrobial agents with activity mainly against Gram-positive strains. The commercial success of linezolid, the only FDA-approved oxazolidinone, has prompted many pharmaceutical companies to devote resources to this area of investigation. Until now, four types of chemical modifications of linezolid and oxazolidinone-type antibacterial agents, including modification on each of the A-(oxazolidinone), B-(phenyl), and C-(morpholine) rings as well as the C-5 side chain of the A-ring substructure, have been described. Division into sections according to side chain modification or the type of ring will be used throughout this review, although the process of synthesis usually involves the simultaneous modification of several elements of the linezolid substructure; therefore, assignment into the appropriate section depends on the structure-activity relationships (SAR) studies. This review makes an attempt to summarise the work carried out in the period from 2006 until mid-2012.
恶唑烷酮类是一类新型且强效的抗菌药物，主要对革兰氏阳性菌具有活性。利奈唑胺（唯一获得 FDA 批准的恶唑烷酮类药物）的商业成功促使许多制药公司投入资源进行这一领域的研究。到目前为止，已经描述了四种对利奈唑胺和恶唑烷酮类抗菌药物的化学修饰，包括对 A-（恶唑烷酮）、B-（苯基）和 C-（吗啉）环以及 A-环亚结构的 C-5 侧链的每个部分的修饰。在本综述中，将根据侧链修饰或环的类型进行划分，尽管合成过程通常涉及利奈唑胺亚结构的几个元素的同时修饰；因此，归入适当的部分取决于结构-活性关系（SAR）研究。本综述试图总结 2006 年至 2012 年年中期间开展的工作。
