Synthesis and Biological Evaluation of 7,8,9,10-Tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as Functionally Selective Ligands of the Benzodiazepine Receptor Site on the GABA_A Receptor

Pamela A Albaugh; Lu Marshall; James Gregory; Geoff White; Alan Hutchison; Phil C. Ross; Dorothy W. Callagher; John F. Tallman; Matt Crago; James V. Cassella

首页> 外文期刊>Journal of Medicinal Chemistry >Synthesis and Biological Evaluation of 7,8,9,10-Tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as Functionally Selective Ligands of the Benzodiazepine Receptor Site on the GABA_A Receptor

【24h】

Synthesis and Biological Evaluation of 7,8,9,10-Tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as Functionally Selective Ligands of the Benzodiazepine Receptor Site on the GABA_A Receptor

机译：GABA_A受体上的二氮杂pine庚因受体功能选择性配体的7,8,9,10-四氢咪唑并[1,2-c]吡啶基[3,4-e] pyrimdin-5（6H）-的合成及生物学评价

获取原文

获取原文并翻译 | 示例

掌桥外文数据库（机构版） >>

开具论文收录证明 >>

文献代查 >>

页面导航

摘要
著录项
相似文献
相关主题

摘要

Benzodiazepines are allosteric modulators of the GABA_A receptor. The traditionally prescribed benzodiazepines are nonselective and suffer from numerous side effects. Upon the identification of receptor subtypes, we set out to discover selective agents with the anticipation that these agents would have superior therapeutic potential. Herein, we describe the synthesis and biological evaluation of substituted 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimidin-5(6H)-ones and disclose that these compounds exhibit functional selectivity at the benzodiazepin receptor of GABA_A receptor subtypes. The α_2/α_3-selective partial agonist 42 exhibited potent in vivo activity.

机译：苯二氮卓类是GABA_A受体的变构调节剂。传统上规定的苯二氮杂类是非选择性的，并且具有许多副作用。在鉴定受体亚型后，我们着手发现选择性药物，并期望这些药物具有更高的治疗潜力。在这里，我们描述了取代的7,8,9,10-四氢咪唑并[1,2-c]吡啶并[3,4-e]嘧啶-5（6H）-的合成及生物学评价，并揭示了这些化合物具有一定的功能。 GABA_A受体亚型对苯并二氮杂receptor受体的选择性。 α_2/α_3-选择性部分激动剂42表现出有效的体内活性。

著录项

来源
《Journal of Medicinal Chemistry》 |2002年第23期|共9页
作者
Pamela A Albaugh; Lu Marshall; James Gregory; Geoff White; Alan Hutchison; Phil C. Ross; Dorothy W. Callagher; John F. Tallman; Matt Crago; James V. Cassella;
展开▼
作者单位

展开▼
收录信息
原文格式 PDF
正文语种 eng
中图分类药学;
关键词

相似文献

外文文献
中文文献
专利

1. Synthesis and Biological Evaluation of 7,8,9,10-Tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as Functionally Selective Ligands of the Benzodiazepine Receptor Site on the GABA_A Receptor [J] . Pamela A Albaugh, Lu Marshall, James Gregory, Journal of Medicinal Chemistry . 2002,第23期

机译：GABA_A受体上的二氮杂pine庚因受体功能选择性配体的7,8,9,10-四氢咪唑并[1,2-c]吡啶基[3,4-e] pyrimdin-5（6H）-的合成及生物学评价
2. Two imidazoquinoxaline ligands for the benzodiazepine site sharing a second low affinity site on rat GABA_A receptors but with the opposite functionality [J] . Haesook K. Im, Wha Bin Im, Jeffrey F.Pregenzer British Journal of Pharmacology . 1998,第8期

机译：苯二氮卓类位点的两个咪唑并喹喔啉配体在大鼠GABA_A受体上共享第二个低亲和力位点，但功能相反
3. 3-Heteroaryl-2-pyridones: Benzodiazepine Site Ligands with Functional Selectivity for α2/α3-Subtypes of Human GABA_A Receptor-Ion Channels [J] . Ian Collins, Christopher Moyes, William B. Davey, Journal of Medicinal Chemistry . 2002,第9期

机译：3-Heteroaryl-2-pyridones：苯二氮卓类配体对人GABA_A受体离子通道的α2/α3-亚型具有功能选择性。
4. Synthesis and biological activity of a new and highly potent ligand for somatostatin receptors 2,3 and 5 [C] . Mihaela Ginj, Damian Wild, Jorg S.Schmitt, European Peptide Symposium . 2002

机译：生长抑素受体2,3和5的新高效配体的合成和生物活性
5. Part One. Synthesis of optically active tryptophan derivatives with potential activity as indoleamine 2,3-dioxygenase inhibitors: An approach via asymmetric catalytic hydrogenation. Part Two. Design, synthesis and pharmacology of selective ligands for alpha1-containing GABA(A)/benzodiazepine receptor subtypes: SAR studies of beta-carbolines at positions -3 and -6 and their corresponding bivalent ligands. Part Three. First enantiospecific total synthesis of the important biogenetic intermediates, (+)-polyneuridine and (+)-polyneuridine aldehyde, as well as 16-epi-vellosimine and macusine A. [D] . Yin, Wenyuan. 2007

机译：第一部分。具有吲哚胺2,3-二加氧酶抑制剂潜在活性的旋光色氨酸衍生物的合成：一种通过不对称催化氢化的方法。第二部分。含α1的GABA（A）/苯并二氮杂receptor受体亚型的选择性配体的设计，合成和药理作用：位于-3和-6位的β-咔啉及其相应的二价配体的SAR研究。第三部分。重要生物遗传中间体，（+）-聚神经氨酸和（+）-聚神经氨酸醛，以及16-表-维西辛和Macusine A的首次对映体全合成。
6. Two imidazoquinoxaline ligands for the benzodiazepine site sharing a second low affinity site on rat GABAA receptors but with the opposite functionality [O] . Haesook K Im, Wha Bin Im, Jeffrey F Pregenzer, 1998

机译：苯二氮卓类位点的两个咪唑并喹喔啉配体在大鼠GABAA受体上共享第二个低亲和力位点但功能相反
7. Design, Synthesis, and Biological Evaluation of Imidazo[1,5‑a]quinoline as Highly Potent Ligands of Central Benzodiazepine Receptors [O] . Andrea Cappelli, Maurizio Anzini, Federica Castriconi, 2016

机译：咪唑并[1,5‑a]喹啉作为中央苯二氮杂Re受体高强度配体的设计，合成及生物学评价

Synthesis and Biological Evaluation of 7,8,9,10-Tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as Functionally Selective Ligands of the Benzodiazepine Receptor Site on the GABA_A Receptor

摘要

著录项

相似文献

相关主题

期刊订阅