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环丙烷同系物的设计与合成E2 型 resolvin，一种内源性的促解决脂质介质，作为其稳定的等价物。

Design and Synthesis of Cyclopropane Congeners of Resolvin E2, an Endogenous Proresolving Lipid Mediator, as Its Stable Equivalents.

机构信息

Faculty of Pharmaceutical Science, Hokkaido University , Kita-12, Nishi-6, Kita-Ku, Sapporo 060-0812, Japan.

出版信息

Org Lett. 2016 Dec 16;18(24):6224-6227. doi: 10.1021/acs.orglett.6b02612. Epub 2016 Nov 28.

DOI:10.1021/acs.orglett.6b02612
PMID:27978690
Abstract

Lipid chemical mediator resolvins with highly potent anti-inflammatory activity can be leads to develop novel anti-inflammatory drugs; however, they are unstable in oxygen due to their characteristic polyunsaturated structures. To solve the problem, CP-RvE2 has been designed and synthesized in which the cis-olefin of RvE2 was replaced with a cyclopropane. CP-RvE2s were much more stable than RvE2 against autoxidation and equipotent or more potent than RvE2. CP-RvE2s were successfully identified as stable equivalents of RvE2.

摘要

具有高效抗炎活性的脂质化学介质消退素可以成为开发新型抗炎药物的先导化合物；然而，由于其特征性的多不饱和结构，它们在氧气中不稳定。为了解决这个问题，设计并合成了 CP-RvE2，其中 RvE2 的顺式烯烃被环丙烷取代。CP-RvE2s 比 RvE2 更稳定，不易自动氧化，与 RvE2 等效或更有效。CP-RvE2s 被成功鉴定为 RvE2 的稳定等价物。

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