Gamma-lactams--a novel scaffold for highly potent and selective alpha7 nicotinic acetylcholine receptor agonists.

Enz A; Feuerbach D; Frederiksen MU; Gentsch C; Hurth K; Muller W; Nozulak J; Roy BL

首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Gamma-lactams--a novel scaffold for highly potent and selective alpha7 nicotinic acetylcholine receptor agonists.

【24h】

Gamma-lactams--a novel scaffold for highly potent and selective alpha7 nicotinic acetylcholine receptor agonists.

机译：γ-内酰胺 - 一种用于高效和选择性α7烟碱乙酰胆碱受体激动剂的新型支架。

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

A novel class of alpha7 nicotinic acetylcholine receptor (nAChR) agonists has been discovered through high-throughput screening. The cis gamma-lactam scaffold has been optimized to reveal highly potent and selective alpha7 nAChR agonists with in vitro activity and selectivity and with good brain penetration in mice.

机译：通过高通量筛选发现了一种新型的α7烟碱乙酰胆碱受体（NACHR）激动剂。已优化CISγ-内酰胺支架，以揭示高效和选择性的α7NACHR激动剂，具有体外活性和选择性，并且在小鼠中良好的脑渗透。

著录项

来源
《Bioorganic and Medicinal Chemistry Letters》 |2009年第5期|共5页
作者
Enz A; Feuerbach D; Frederiksen MU; Gentsch C; Hurth K; Muller W; Nozulak J; Roy BL;
展开▼
作者单位

Novartis Institutes for Biomedical Research Neuroscience Disease Area 4002 Basel Switzerland.;

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. Gamma-lactams--a novel scaffold for highly potent and selective alpha7 nicotinic acetylcholine receptor agonists. [J] . Enz A, Feuerbach D, Frederiksen MU, Bioorganic and Medicinal Chemistry Letters . 2009,第5期

机译：γ-内酰胺 - 一种用于高效和选择性α7烟碱乙酰胆碱受体激动剂的新型支架。
2. Role of alpha7 nicotinic acetylcholine receptors in regulating tumor necrosis factor-alpha (TNF-alpha) as revealed by subtype selective agonists. [J] . Li J, Mathieu SL, Harris R, Journal of Neuroimmunology: Official Bulletin of the Research Committee on Neuroimmunology of the World Federation of Neurology . 2011,第1a2期

机译：亚型选择性激动剂揭示了α7烟碱型乙酰胆碱受体在调节肿瘤坏死因子-α（TNF-α）中的作用。
3. Synthesis and SAR studies of 1,4-diazabicyclo(3.2.2)nonane phenyl carbamates--subtype selective, high affinity alpha7 nicotinic acetylcholine receptor agonists. [J] . ODonnell CJ, Peng L, ONeill BT Bioorganic and Medicinal Chemistry Letters . 2009,第16期

机译：1,4-二氮杂双环（3.2.2）壬烷苯基氨基甲酸酯的合成和SAR研究-亚型选择性高亲和力α7烟碱乙酰胆碱受体激动剂。
4. Regulation of Dopamine Release by Striatal Acetylcholine and Nicotine Is via Distinct Nicotinic Acetylcholine Receptors in Dorsal vs. Ventral Striatum [C] . Richard Exley, Michael A. Clements, Stephanie J. Cragg Triennial Meeting of the International Basal Ganglia Society . 2009

机译：通过纹状体乙酰胆碱和尼古丁对多巴胺释放的调节是通过不同的烟碱乙酰胆碱受体在背侧与腹侧纹状体中
5. Approaches in Developing Selective Pharmacological Lead Compounds for the alpha7 Nicotinic Acetylcholine Receptor with Click-Chemistry [D] . Yamauchi, John G. 2012

机译：用点击化学方法开发用于α7烟碱乙酰胆碱受体的选择性药理先导化合物的方法
6. Discovery of Highly Potent and Selective α4β2-Nicotinic Acetylcholine Receptor (nAChR) Partial Agonists Containing an Isoxazolylpyridine Ether Scaffold that Demonstrate Antidepressant-like Activity. Part II [O] . Li-Fang Yu, J. Brek Eaton, Allison Fedolak, -1

机译：高度有效的和选择性α4β2烟碱乙酰胆碱受体（naChR的）部分激动剂包含一个Isoxazolylpyridine以太脚手架演示抗抑郁样活性的发现。第二部分
7. Discovery of the a7 Nicotinic Acetylcholine Receptor Agonists. (R)-3-(5-Chlorothiophen-2-yl)spiro-1-azabicyclo2.2.2octane-3, 5-1, 3oxazolidin-2-one as a Novel, Potent, Selective, and Orally Bioavailable Ligand [O] . -1

机译：发现A7烟碱乙酰胆碱受体激动剂。（r）-3-（5-氯噻吩-2-基）螺旋-1- azabocyclo 2.2.2辛烷-3，5- 1,3恶唑烷-2-单，为新型，有效，选择性和口服生物可利用的配体
8. Use of Monoclonal Antibodies to Study the Structural Basis of the Function of Nicotinic Acetylcholine Receptors on Electric Organ and Muscle and to Determine the Structure of Nicotinic Acetylcholine Receptors on Neurons. [R] . Lindstrom, J. M. 1989

机译：使用单克隆抗体研究烟碱型乙酰胆碱受体在电活动器官和肌肉上的功能结构基础，并确定神经元上烟碱型乙酰胆碱受体的结构。

Gamma-lactams--a novel scaffold for highly potent and selective alpha7 nicotinic acetylcholine receptor agonists.

摘要

著录项

相似文献

相关主题

期刊订阅