Structure-activity relationship studies on 1-(2-(4-Phenylphenoxy)ethyl)pyrrolidine (SC-22716), a potent inhibitor of leukotriene A(4) (LTA(4)) hydrolase.

Penning TD; Chandrakumar NS; Chen BB; Chen HY; Desai BN; Djuric SW; Docter SH; Gasiecki AF; Haack RA; Miyashiro JM; Russell MA; Yu SS; Corley DG; Durley RC; Kilpatrick BF; Parnas BL; Askonas LJ; Gierse JK; Harding EI; Highkin MK; Kachur JF; Kim SH; Krivi GG; Villani Price-D; Pyla EY; Smith WG

首页> 外文期刊>Journal of Medicinal Chemistry >Structure-activity relationship studies on 1-(2-(4-Phenylphenoxy)ethyl)pyrrolidine (SC-22716), a potent inhibitor of leukotriene A(4) (LTA(4)) hydrolase.

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Structure-activity relationship studies on 1-(2-(4-Phenylphenoxy)ethyl)pyrrolidine (SC-22716), a potent inhibitor of leukotriene A(4) (LTA(4)) hydrolase.

机译：结构-活性关系研究1-（2-（4-苯基苯氧基）乙基）吡咯烷（SC-22716），白三烯A（4）（LTA（4））水解酶的有效抑制剂。

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Leukotriene B(4) (LTB(4)) is a pro-inflammatory mediator that has been implicated in the pathogenesis of a number of diseases including inflammatory bowel disease (IBD) and psoriasis. Since the action of LTA(4) hydrolase is the rate-limiting step for LTB(4) production, this enzyme represents an attractive pharmacological target for the suppression of LTB(4) production. From an in-house screening program, SC-22716 (1, 1-[2-(4-phenylphenoxy)ethyl]pyrrolidine) was identified as a potent inhibitor of LTA(4) hydrolase. Structure-activity relationship (SAR) studies around this structural class resulted in the identification of a number of novel, potent inhibitors of LTA(4) hydrolase, several of which demonstrated good oral activity in a mouse ex vivo whole blood assay.

机译：白三烯B（4）（LTB（4））是促炎性介质，已与包括炎症性肠病（IBD）和牛皮癣在内的多种疾病的发病机制有关。由于LTA（4）水解酶的作用是LTB（4）生产的限速步骤，因此该酶代表了抑制LTB（4）生产的诱人药理学目标。通过内部筛选程序，SC-22716（1，1- [2-（4-苯基苯氧基）乙基]吡咯烷）被确定为LTA（4）水解酶的有效抑制剂。围绕此结构类别的结构活性关系（SAR）研究导致鉴定了许多新型的，有效的LTA（4）水解酶抑制剂，其中几种在小鼠离体全血试验中表现出良好的口服活性。

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来源
《Journal of Medicinal Chemistry》 |2000年第4期|共15页
作者
Penning TD; Chandrakumar NS; Chen BB; Chen HY; Desai BN; Djuric SW; Docter SH; Gasiecki AF; Haack RA; Miyashiro JM; Russell MA; Yu SS; Corley DG; Durley RC; Kilpatrick BF; Parnas BL; Askonas LJ; Gierse JK; Harding EI; Highkin MK; Kachur JF; Kim SH; Krivi GG; Villani Price-D; Pyla EY; Smith WG;
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正文语种 eng
中图分类药学;
关键词
Enzyme Inhibitors; Epoxide Hydrolases; Pyrrolidines; leukotriene A4-hydrolase; 酶抑制剂; 环氧水解酶类; 吡咯烷类;

机译：Enzyme Inhibitors;Epoxide Hydrolases;Pyrrolidines;leukotriene A4-hydrolase;酶抑制剂;环氧水解酶类;吡咯烷类;

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1. Structure-activity relationship studies on 1-(2-(4-Phenylphenoxy)ethyl)pyrrolidine (SC-22716), a potent inhibitor of leukotriene A(4) (LTA(4)) hydrolase. [J] . Penning TD, Chandrakumar NS, Chen BB, Journal of Medicinal Chemistry . 2000,第4期

机译：结构-活性关系研究1-（2-（4-苯基苯氧基）乙基）吡咯烷（SC-22716），白三烯A（4）（LTA（4））水解酶的有效抑制剂。
2. Potent and selective ligands for the dopamine transporter (DAT): structure-activity relationship studies of novel 4-(2-(diphenylmethoxy)ethyl)-1-(3-phenylpropyl)piperidine analogues. [J] . Dutta AK, Coffey LL, Reith ME Journal of Medicinal Chemistry . 1998,第5期

机译：多巴胺转运蛋白（DAT）的有效和选择性配体：新型4-（2-（二（苯基苯甲氧基）乙基）-1-（3-苯基丙基）哌啶类似物的结构-活性关系研究。
3. Structure-activity relationship studies of highly selective inhibitors of the dopamine transporter: N-benzylpiperidine analogues of 1-(2-(bis(4-fluorophenyl)methoxy)ethyl)-4-(3-phenylpropyl)piperazine. [J] . Greiner E, Prisinzano T, Johnson II EM, Journal of Medicinal Chemistry . 2003,第8期

机译：多巴胺转运蛋白的高选择性抑制剂的结构活性关系研究：1-（2-（双（4-（4-氟苯基）甲氧基）乙基）-4-（3-苯丙基）哌嗪的N-苄基哌啶类似物。
4. Synthesis and Structure-Activity Relationship Studies of Cryptophycins: A Novel Class of Potent Antimitotic Antitumor Depsipeptides [C] . Chuan Shih, Rima S. Al-Awar, Andrew H. Fray, American Chemical Society . 2001

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7. Group-based optimization of potent and cell-active inhibitors of the von Hippel-Lindau (VHL) E3 ubiquitin ligase:structure-activity relationships leading to the chemical probe (2S,4R)-1-((S)-2-(1-cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (VH298) [O] . Soares Pedro, Gadd Morgan, Frost Julianty, 2017

机译：基于组的von Hippel-Lindau（VHL）E3泛素连接酶有效和细胞活性抑制剂的优化：结构-活性关系导致化学探针（2S，4R）-1-（（S）-2-（1 -氰基环丙烷甲酰胺基）-3,3-二甲基丁酰基）-4-羟基-N-（4-（4-甲基噻唑-5-基）苄基）吡咯烷-2-羧酰胺（VH298）

Structure-activity relationship studies on 1-(2-(4-Phenylphenoxy)ethyl)pyrrolidine (SC-22716), a potent inhibitor of leukotriene A(4) (LTA(4)) hydrolase.

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