Gravestock Michael B
Infection Discovery, AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA.
Curr Opin Drug Discov Devel. 2005 Jul;8(4):469-77.
The oxazolidinone antibacterials represent an unusual example of a new synthetic class of compounds for the treatment of drug-resistant Gram-positive infections. The first clinically approved example of this class is linezolid, which, despite showing considerable clinical promise, can cause side effects that prevent general use of the drug in the community. New research has been directed toward broadening the antibacterial spectrum of this class of compound, re-establishing sensitivity to linezolid-resistant strains and lowering the toxicity potential. This research has yielded new bioisosteres of the oxazolidinone ring and, in another approach, created hybrid structures with existing Gram-negative active drug classes. New oxazolidinone-based drugs are in early clinical development and indications are that this class of antibacterials will continue to show promise.
恶唑烷酮类抗菌药物是用于治疗耐药革兰氏阳性菌感染的新型合成化合物类别的一个不同寻常的例子。该类别首个获得临床批准的药物是利奈唑胺，尽管它展现出了可观的临床前景，但会引起一些副作用，这使得该药物无法在社区广泛使用。新的研究致力于拓宽这类化合物的抗菌谱，恢复对利奈唑胺耐药菌株的敏感性，并降低潜在毒性。这项研究已产生了恶唑烷酮环的新生物电子等排体，并且，从另一种方法来看，还创造出了与现有的对革兰氏阴性菌有活性的药物类别形成的杂合结构。基于恶唑烷酮的新型药物正处于临床早期开发阶段，种种迹象表明这类抗菌药物将继续展现出前景。
