Design and Synthesis of Cyclopropane Congeners of Resolvin E2, an Endogenous Proresolving Lipid Mediator, as Its Stable Equivalents
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- 作者：Hayato Fukuda ; Ryuta Muromoto ; Yuuki Takakura ; Kohei Ishimura ; Ryutaro Kanada ; Daichi Fushihara ; Makoto Tanabe ; Kotaro Matsubara ; Toru Hirao ; Koki Hirashima ; Hiroshi Abe ; Mitsuhiro Arisawa ; Tadashi Matsuda ; Satoshi Shuto
- 刊名：Organic Letters
- 出版年：2016
- 出版时间：December 16, 2016
- 年：2016
- 卷：18
- 期：24
- 页码：6224-6227
- 全文大小：370K
- ISSN：1523-7052
文摘
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.