Discovery of enantioselectivity of urea inhibitors of soluble epoxide hydrolase
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- 作者：Manoj Manickama ; Thanigaimalai Pillaiyara ; PullaReddy Boggua ; Eeda Venkateswararaoa ; Hitesh B. Jalania ; Nam-Doo Kimb ; Seul Ki Leea ; Jang Su Jeona ; Sang Kyum Kima ; Sang-Hun Junga ; jungshh@cnu.ac.kr" class="auth_mail" title="E-mail the corresponding author
- 关键词：EETs ; Soluble epoxide hydrolase ; Inhibitors ; Urea derivatives ; Enantioselectivity
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：19 July 2016
- 年：2016
- 卷：117
- 期：Complete
- 页码：113-124
- 全文大小：3752 K
文摘
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Enantioselective 1-(α-alkyl-α-phenylmethyl)-3-(3-phenylpropyl)urea inhibitor of soluble epoxide hydrolase was discovered.
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The S-isomer of 8e showed 125 fold more active than its R-isomer.
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Restriction of the free rotation of two α-groups with fused bicyclic moiety abolishes the selectivity.
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These urea analogs are specific inhibitor of sEH without inhibition of mEH.