Synthesis and SAR of 3- and 4-substituted quinolin-2-ones: discovery of mixed 5-HT(1B)/5-HT(2A) receptor antagonists.

McCort G; Hoornaert C; Aletru M; Denys C; Duclos O; Cadilhac C; Guilpain E; Dellac G; Janiak P; Galzin AM; Delahaye M; Guilbert F; OConnor S

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Synthesis and SAR of 3- and 4-substituted quinolin-2-ones: discovery of mixed 5-HT(1B)/5-HT(2A) receptor antagonists.

机译：3-和4-取代的喹啉-2-酮的合成和合成孔径雷达：混合的5-HT（1B）/ 5-HT（2A）受体拮抗剂的发现。

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Quinolin-2-ones bearing a heteroaryl-piperazine linked by a two carbon chain at the 3- or 4-position were synthesised and evaluated as mixed 5-HT(1B)/5-HT(2A) receptor antagonists. Potent mixed antagonists were obtained with thieno[3,2-c]pyridine derivatives. In this series, compound 2.1 (SL 65.0472) proved to be functional antagonist at both the 5-HT(2A) receptor (rat in vivo 5-HT-induced hypertension model) and the 5-HT(1B) receptor (dog in vitro saphenous vein assay).

机译：合成了在3或4位上带有通过两个碳链连接的杂芳基-哌嗪的喹啉-2-酮，并将其评估为混合的5-HT（1B）/ 5-HT（2A）受体拮抗剂。用噻吩并[3,2-c]吡啶衍生物获得有效的混合拮抗剂。在这个系列中，化合物2.1（SL 65.0472）被证明是5-HT（2A）受体（大鼠体内5-HT诱发的高血压模型）和5-HT（1B）受体（狗体外）的功能拮抗剂隐静脉测定）。

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《Bioorganic and medicinal chemistry》 |2001年第8期|共9页
作者
McCort G; Hoornaert C; Aletru M; Denys C; Duclos O; Cadilhac C; Guilpain E; Dellac G; Janiak P; Galzin AM; Delahaye M; Guilbert F; OConnor S;
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正文语种 eng
中图分类药学;生物化学;
关键词
Piperazines; Quinolines; Receptors; Serotonin; Serotonin Antagonists; 7-fluoro-2-oxo-4-(2-(4-(thieno(3; 2-c)pyridin-4-yl)piperazin-1-yl)ethyl)-1; 2-dihydroquinoline-1-acetamide; 哌嗪类; 喹啉类; 受体; 血清素; 血清素拮抗药;

机译：Piperazines;Quinolines;Receptors;Serotonin;Serotonin Antagonists;7-fluoro-2-oxo-4-(2-(4-(thieno(3;2-c)pyridin-4-yl)piperazin-1-yl)ethyl)-1;2-dihydroquinoline-1-acetamide;哌嗪类;喹啉类;受体;血清素;血清素拮抗药;

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1. Synthesis and SAR of 3- and 4-substituted quinolin-2-ones: discovery of mixed 5-HT(1B)/5-HT(2A) receptor antagonists. [J] . McCort G, Hoornaert C, Aletru M, Bioorganic and medicinal chemistry . 2001,第8期

机译：3-和4-取代的喹啉-2-酮的合成和合成孔径雷达：混合的5-HT（1B）/ 5-HT（2A）受体拮抗剂的发现。
2. Microwave assisted synthesis of 2-(4-substituted piperazin-1-yl)-1,8-naphthyridine-3-carbonitrile as a new class of serotonin 5-HT(3) receptor antagonists. [J] . Mahesh R, Venkatesha Perumal R, Vijaya Pandi P Bioorganic and Medicinal Chemistry Letters . 2004,第20期

机译：微波辅助合成2-（4-取代的哌嗪-1-基）-1,8-萘啶-3-甲腈作为新型的5-羟色胺5-HT（3）受体拮抗剂。
3. Synthesis and biological evaluation of (phenylpiperazinyl-propyl)arylsulfonamides as selective 5-HT(2A) receptor antagonists. [J] . Yoo E, Yoon J, Pae A Bioorganic and medicinal chemistry . 2010,第4期

机译：作为选择性5-HT（2A）受体拮抗剂的（苯基哌嗪基-丙基）芳基磺酰胺的合成和生物学评估。
4. 5-HT_7 Receptor-Mediated Meningeal Dilatation Induced by 5-Carboxamidotryptamine in Rats is Not Altered by 5-HT Depletion and Chronic Corticosterone Treatment [C] . Martinez-Garcia E., Sanchez-Maldonado C. Terron J.A. Western Pharmacology Society . 2011

机译：5-HT_7受体介导的5-羧胺酰胺肽在大鼠中诱导的大鼠诱导的脑膜扩张不会通过5-HT耗尽和慢性皮质酮处理来改变
5. A 5-HT locomotor system: Identification, actions through 5-HT(2A/7) receptor subtypes, and effects on the control of locomotion. [D] . Liu, Jun. 2007

机译：5-HT运动系统：识别，通过5-HT（2A / 7）受体亚型的作用，以及对运动控制的影响。
6. Excessive Activation of Serotonin (5-HT) 1B Receptors Disrupts the Formation of Sensory Maps in Monoamine Oxidase A and 5-HT Transporter Knock-Out Mice [O] . Nathalie Salichon, Patricia Gaspar, A. Louise Upton, 2001

机译：血清素（5-HT）1B受体的过度激活破坏了单胺氧化酶A和5-HT转运蛋白敲除小鼠的感觉图谱的形成。
7. Synthesis and activity of functionalizable derivatives of the serotonin (5-HT) 5-HT 2A receptor (5-HT 2A R) antagonist M100907 [O] . Scott R. Gilbertson, Ying-Chu Chen, Claudia A. Soto, 2018

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Synthesis and SAR of 3- and 4-substituted quinolin-2-ones: discovery of mixed 5-HT(1B)/5-HT(2A) receptor antagonists.

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