Synthesis and serotonergic activity of variously substituted (3-amido)phenylpiperazine derivatives and benzothiophene-4-piperazine derivatives: novel antagonists for the vascular 5-HT1B receptor.

Moloney GP; Garavelas A; Martin GR; Maxwell M; Glen RC

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Synthesis and serotonergic activity of variously substituted (3-amido)phenylpiperazine derivatives and benzothiophene-4-piperazine derivatives: novel antagonists for the vascular 5-HT1B receptor.

机译：各种取代的（3-氨基）苯基哌嗪衍生物和苯并噻吩-4-哌嗪衍生物的合成和血清素能活性：血管5-HT1B受体的新型拮抗剂。

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The synthesis and vascular 5-HT(1B) receptor activity of a novel series of substituted 3-amido phenylpiperazine and 4-(4-methyl-1-piperazinyl)-1-benzo[b]thiophene derivatives is described. Modifications to the amido linked sidechains of the 3-amidophenyl-piperazine derivatives and to the 2-sidechain of the 1-benzo[b]thiophene derivatives have been explored. Several compounds were identified which exhibited affinity at the vascular 5-HT(1B) receptor of pK(B) > 7.0. From the 3-amidophenyl-piperazine series, N-(4-(4-chlorophenyl)thiazol-2-yl-3-(4-methyl-1-piperazinyl)benzamide (30) and from the benzo[b]thiophene-4-piperazine series N-(2-ethylphenyl)-4-(4-methyl-1- piperazinyl)-1-benzo[b]thiophene-2-carboxamide (38) were identified as a highly potent, silent (as judged by the inability of angiotensin II to unmask 5-HT(1B) receptor mediated agonist activity in the rabbit femoral artery) and competitive vascular 5-HT(1B) receptor antagonist. The affinity of compounds from these two series of compounds for the vascular 5-HT(1B) receptor is discussed as well as a proposed mode of binding to the receptor pharmacophore.

机译：描述了一系列新的取代的3-酰胺基苯基哌嗪和4-（4-甲基-1-哌嗪基）-1-苯并[b]噻吩衍生物的合成和血管5-HT（1B）受体活性。已经研究了对3-酰胺基苯基-哌嗪衍生物的酰胺基连接的侧链和1-苯并[b]噻吩衍生物的2-侧链的修饰。鉴定出对pK（B）> 7.0的血管5-HT（1B）受体表现出亲和力的几种化合物。由3-氨基苯基-哌嗪系列，N-（4-（4-氯苯基）噻唑-2-基-3-（4-甲基-1-哌嗪基）苯甲酰胺（30）和苯并[b]噻吩-4 -哌嗪系列N-（2-乙基苯基）-4-（4-甲基-1-哌嗪基）-1-苯并[b]噻吩-2-羧酰胺（38）被鉴定为高效，沉默的药物（根据血管紧张素II不能消除5-HT（1B）受体介导的兔股动脉激动剂活性和竞争性血管5-HT（1B）受体拮抗剂的作用。这两个系列化合物对血管5-HT的亲和力讨论了（1B）受体以及与受体药效团结合的提议模式。

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来源
《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2004年第4期|共17页
作者
Moloney GP; Garavelas A; Martin GR; Maxwell M; Glen RC;
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正文语种 eng
中图分类基础医学;
关键词
serotonin 1B receptor; derivatives; Blood vascular; piperazine; Thiophene;

机译：血清素1B受体;衍生物;血管;哌嗪;噻吩;

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1. Synthesis and serotonergic activity of variously substituted (3-amido)phenylpiperazine derivatives and benzothiophene-4-piperazine derivatives: novel antagonists for the vascular 5-HT1B receptor. [J] . Moloney GP, Garavelas A, Martin GR, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2004,第4期

机译：各种取代的（3-氨基）苯基哌嗪衍生物和苯并噻吩-4-哌嗪衍生物的合成和血清素能活性：血管5-HT1B受体的新型拮抗剂。
2. Synthesis and serotonergic activity of substituted 2, N-benzylcarboxamido-5-(2-ethyl-1-dioxoimidazolidinyl)-N, N-dimethyltryptamine derivatives: novel antagonists for the vascular 5-HT(1B)-like receptor. [J] . Moloney GP, Martin GR, Mathews N, Journal of Medicinal Chemistry . 1999,第14期

机译：取代的2，N-苄基羧酰胺基-5-（2-乙基-1-二氧代咪唑啉基）-N，N-二甲基色胺衍生物的合成和血清素能活性：血管5-HT（1B）-样受体的新型拮抗剂。
3. Synthesis and serotonergic activity of a series of 2-(N-benzyl)-carboxamido-5-substituted-N, N-dimethyltryptamine derivatives: novel antagonists for the vascular 5-HT_(1B)-like receptors [J] . Gerard P. Moloney, Graeme R. Martin, Neil Mathews, Journal of the Chemical Society, Perkin Transactions 1 . 1999,第19期

机译：一系列的2-（N-苄基）-羧酰胺基-5-取代的N，N-二甲基色胺衍生物的合成和血清素能活性：血管5-HT_（1B）-样受体的新型拮抗剂
4. BIOMIMETIC ELECTROCHEMICAL SYNTHESIS OF QUINOL-THIOETHER CONJUGATES : THEIR IMPLICATION IN THE SEROTONERGIC NEUROTOXICITY OF AMPHETAMINE DERIVATIVES [C] . ANNE NEUDORFFER, JEAN-PIERRE GRAMOND, CYRINE SLIM, The Meeting of the Electrochemical Society . 2003

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机译：I.取代2-氧杂双环（3.2.1）正己烷衍生物的合成方法和II。合成1-取代的酸酐（3-氯乙酰基-2-羟基咪唑并（1,2-A）吡啶鎓氢氧化物）。
6. Synthesis and Anti-Intestinal Nematode Activity of Variously Substituted Benzonaphthyridine Derivatives [O] . Li-Ping Duan, Ai-Dan Wen, Ning-Bo Wu, 2011

机译：各种取代的苯并萘啶衍生物的合成及抗肠道线虫活性
7. Synthesis and Anti-Intestinal Nematode Activity of Variously Substituted Benzonaphthyridine Derivatives [O] . Ai-Dan Wen, Yi Tao, Ning-Bo Wu, 2011

机译：不同取代苯并萘啶衍生物的合成及抗肠道线虫活性

Synthesis and serotonergic activity of variously substituted (3-amido)phenylpiperazine derivatives and benzothiophene-4-piperazine derivatives: novel antagonists for the vascular 5-HT1B receptor.

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