Solid-phase combinatorial approach for the optimization of soluble epoxide hydrolase inhibitors.

Hwang SH; Morisseau C; Do Z; Hammock BD

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Solid-phase combinatorial approach for the optimization of soluble epoxide hydrolase inhibitors.

机译：固相组合法优化可溶性环氧化物水解酶抑制剂。

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A 192-member library of N,N'-disubstituted urea inhibitors was synthesized by a solid-phase method. The ureas were tested for their inhibitory activities against recombinant human soluble epoxide hydrolase. Simple carbocyclic or para/meta-substituted phenyl groups showed inhibition potencies that were equal to or greater than adamantane-based sEH inhibitors, while the presence of bulky or ionizable groups close to the urea group dramatically decreased their activities.

机译：通过固相法合成了192个N，N′-二取代脲抑制剂的文库。测试了脲对重组人可溶性环氧化物水解酶的抑制活性。简单的碳环或对位/对位取代的苯基基团显示出等于或大于基于金刚烷的sEH抑制剂的抑制能力，而靠近尿素基团的大体积或可电离基团的存在大大降低了它们的活性。

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《Bioorganic and Medicinal Chemistry Letters》 |2006年第22期|共5页
作者
Hwang SH; Morisseau C; Do Z; Hammock BD;
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正文语种 eng
中图分类基础医学;
关键词
inhibitors; Solid; Epoxide Hydrolases; Urea; 环氧水解酶类; 尿素;

机译：inhibitors;Solid;Epoxide Hydrolases;Urea;环氧水解酶类;尿素;

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1. Solid-phase combinatorial approach for the optimization of soluble epoxide hydrolase inhibitors. [J] . Hwang SH, Morisseau C, Do Z, Bioorganic and Medicinal Chemistry Letters . 2006,第22期

机译：固相组合法优化可溶性环氧化物水解酶抑制剂。
2. Non-urea functionality as the primary pharmacophore in soluble epoxide hydrolase inhibitors. [J] . Anandan SK, Do ZN, Webb HK, Bioorganic and Medicinal Chemistry Letters . 2009,第4期

机译：非脲官能团是可溶性环氧化物水解酶抑制剂中的主要药效团。
3. A strategy of employing aminoheterocycles as amide mimics to identify novel, potent and bioavailable soluble epoxide hydrolase inhibitors. [J] . Shen HC, Ding FX, Deng Q Bioorganic and Medicinal Chemistry Letters . 2009,第19期

机译：使用氨基杂项作为酰胺模拟物的策略，以鉴定新型，有效和生物可利用的可溶性环氧化物水解酶抑制剂。
4. INHIBITION OF EPOXIDE HYDROLASES AND GLUTATHIONE S-TRANSFERASE BY 2-, 3- AND 4-SUBSTITUTED DERIVATIVES OF 4-PHENYLCHALCONE AND ITS EPOXIDE [C] . T. Miyamoto, M. Sylva, B.D. Hammock International Congress of Pesticide Chemistry . 1986

机译：抑制环氧化物水解酶和谷胱甘肽S转移酶的2-，3-和4-取代的4-苯基凝块及其环氧化物的衍生物
5. Combinatorial Treatment of Diazepam and Soluble Epoxide Hydrolase Inhibition Stops Seizures and Modulates the Neuroinflammatory Response in a Murine Model of TETS Intoxication. [D] . Vito, Stephen Thomas. 2014

机译：地西p和可溶性环氧化物水解酶抑制的组合治疗可阻止癫痫发作并调节TETS中毒小鼠模型的神经炎症反应。
6. Solid-phase combinatorial approach for the optimization of soluble epoxide hydrolase inhibitors [O] . Sung Hee Hwang, Christophe Morisseau, Zung Do, -1

机译：固相组合法优化可溶性环氧水解酶抑制剂
7. Solid-phase combinatorial approach for the optimization of soluble epoxide hydrolase inhibitors [O] . Sung Hee Hwang, Christophe Morisseau, Zung Do, 2006

机译：可溶性环氧化物水解酶抑制剂优化的固相组合方法

Solid-phase combinatorial approach for the optimization of soluble epoxide hydrolase inhibitors.

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