万古霉素相关糖肽类抗生素及关键类似物的全合成
Total Syntheses of Vancomycin-Related Glycopeptide Antibiotics and Key Analogues.
作者信息
Okano Akinori, Isley Nicholas A, Boger Dale L
机构信息
Department of Chemistry and the Skaggs Institute for Chemical Biology, The Scripps Research Institute , 10550 North Torrey Pines Road, La Jolla, California 92037, United States.
出版信息
Chem Rev. 2017 Sep 27;117(18):11952-11993. doi: 10.1021/acs.chemrev.6b00820. Epub 2017 Apr 24.
Abstract
A review of efforts that have provided total syntheses of vancomycin and related glycopeptide antibiotics, their agylcons, and key analogues is provided. It is a tribute to developments in organic chemistry and the field of organic synthesis that not only can molecules of this complexity be prepared today by total synthesis but such efforts can be extended to the preparation of previously inaccessible key analogues that contain deep-seated structural changes. With the increasing prevalence of acquired bacterial resistance to existing classes of antibiotics and with the emergence of vancomycin-resistant pathogens (VRSA and VRE), the studies pave the way for the examination of synthetic analogues rationally designed to not only overcome vancomycin resistance but provide the foundation for the development of even more powerful and durable antibiotics.
摘要
本文综述了全合成万古霉素及相关糖肽抗生素、其苷元及关键类似物的研究工作。这体现了有机化学和有机合成领域的发展成果，如今不仅能够通过全合成制备如此复杂的分子，还能将此类研究扩展至制备此前难以获得的、具有深层次结构变化的关键类似物。随着获得性细菌对现有抗生素类别的耐药性日益普遍，以及耐万古霉素病原体（VRSA和VRE）的出现，这些研究为合理设计合成类似物奠定了基础，这些类似物不仅能克服万古霉素耐药性，还为开发更强大、更持久的抗生素提供了依据。
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