• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

新型代谢型谷氨酸受体5拮抗剂的杂双环模板的发现。

Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists.

作者信息

Kulkarni Santosh S, Newman Amy Hauck

机构信息

Medicinal Chemistry Section, National Institute on Drug Abuse, Intramural Research Program, NIH, DHHS, Baltimore, MD 21224, USA.

出版信息

Bioorg Med Chem Lett. 2007 Jun 1;17(11):2987-91. doi: 10.1016/j.bmcl.2007.03.066. Epub 2007 Mar 24.

DOI:10.1016/j.bmcl.2007.03.066
PMID:17446071
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1973162/
Abstract

Investigation of a series of heterobicyclic compounds with essential pharmacophoric features of the metabotropic glutamate receptor 5 (mGluR5) antagonists MPEP and MTEP provided novel structural templates with sub-micromolar affinities at the mGluR5.

摘要

对一系列具有代谢型谷氨酸受体5（mGluR5）拮抗剂MPEP和MTEP基本药效基团特征的杂环化合物进行研究，得到了对mGluR5具有亚微摩尔亲和力的新型结构模板。

相似文献

1
Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists.新型代谢型谷氨酸受体5拮抗剂的杂双环模板的发现。
Bioorg Med Chem Lett. 2007 Jun 1;17(11):2987-91. doi: 10.1016/j.bmcl.2007.03.066. Epub 2007 Mar 24.
2
Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.3-[(2-甲基-1,3-噻唑-4-基)乙炔基]吡啶类似物作为强效、非竞争性代谢型谷氨酸受体5拮抗剂的合成及其构效关系；寻找可卡因治疗药物。
J Med Chem. 2006 Feb 9;49(3):1080-100. doi: 10.1021/jm050570f.
3
Neuroprotective activity of the mGluR5 antagonists MPEP and MTEP against acute excitotoxicity differs and does not reflect actions at mGluR5 receptors.代谢型谷氨酸受体5（mGluR5）拮抗剂2-甲基-6-（苯乙炔基）吡啶（MPEP）和2-甲基-6-（2-噻吩乙炔基）吡啶（MTEP）对急性兴奋性毒性的神经保护活性存在差异，且并不反映其对mGluR5受体的作用。
Br J Pharmacol. 2005 Jun;145(4):527-34. doi: 10.1038/sj.bjp.0706219.
4
Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS.通过功能高通量筛选鉴定的新型非 MPEP 化学型 mGluR5 NAMs 的合成和 SAR 研究。
Bioorg Med Chem Lett. 2009 Dec 1;19(23):6502-6. doi: 10.1016/j.bmcl.2009.10.059. Epub 2009 Oct 28.
5
Metabotropic glutamate receptor subtype 5 antagonists MPEP and MTEP.代谢型谷氨酸受体5亚型拮抗剂MPEP和MTEP。
CNS Drug Rev. 2006 Summer;12(2):149-66. doi: 10.1111/j.1527-3458.2006.00149.x.
6
The antinociceptive and anxiolytic-like effects of the metabotropic glutamate receptor 5 (mGluR5) antagonists, MPEP and MTEP, and the mGluR1 antagonist, LY456236, in rodents: a comparison of efficacy and side-effect profiles.代谢型谷氨酸受体5（mGluR5）拮抗剂MPEP和MTEP以及mGluR1拮抗剂LY456236在啮齿动物中的抗伤害感受和抗焦虑样作用：疗效和副作用特征比较
Psychopharmacology (Berl). 2005 Apr;179(1):207-17. doi: 10.1007/s00213-005-2143-4. Epub 2005 Jan 29.
7
Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series.强效 mGluR5 拮抗剂：吡啶基和噻唑基-乙炔基-3,5-二取代-苯基系列。
Bioorg Med Chem Lett. 2011 Jun 1;21(11):3243-7. doi: 10.1016/j.bmcl.2011.04.047. Epub 2011 Apr 20.
8
Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists.将N-(6-甲基吡啶基)取代的芳基酰胺与2-甲基-6-(取代芳基乙炔基)吡啶或2-甲基-4-(取代芳基乙炔基)噻唑作为新型代谢型谷氨酸受体亚型5拮抗剂进行构效关系比较。
J Med Chem. 2009 Jun 11;52(11):3563-75. doi: 10.1021/jm900172f.
9
Behavioral and functional evidence of metabotropic glutamate receptor 2/3 and metabotropic glutamate receptor 5 dysregulation in cocaine-escalated rats: factor in the transition to dependence.可卡因递增大鼠中代谢型谷氨酸受体 2/3 和代谢型谷氨酸受体 5 失调的行为和功能证据：向依赖过渡的因素。
Biol Psychiatry. 2010 Aug 1;68(3):240-8. doi: 10.1016/j.biopsych.2010.02.011. Epub 2010 Apr 22.
10
Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5.新型 7-取代芳基喹啉和 5-取代芳基苯并噻唑类代谢型谷氨酸受体 5 亚型的构效关系。
Bioorg Med Chem. 2010 May 1;18(9):3026-35. doi: 10.1016/j.bmc.2010.03.053. Epub 2010 Mar 27.

引用本文的文献

1
A Simple Precursor for Highly Functionalized Fused Imidazo[4,5-b]pyridines and Imidazo[4,5-b]-1,8-naphthyridine.一种用于高度官能化稠合咪唑并[4,5-b]吡啶和咪唑并[4,5-b]-1,8-萘啶的简单前体。
Molecules. 2016 Dec 1;21(12):1646. doi: 10.3390/molecules21121646.
2
N-(6-Chloro-1-methyl-1H-imidazo[4,5-c]pyridin-4-yl)benzene-sulfonamide.N-（6-氯-1-甲基-1H-咪唑并[4,5-c]吡啶-4-基）苯磺酰胺
Acta Crystallogr Sect E Struct Rep Online. 2014 Mar 15;70(Pt 4):o445. doi: 10.1107/S1600536814005388. eCollection 2014 Apr 1.
3
1-(6-Chloro-1-methyl-1H-imidazo[4,5-c]pyridin-4-yl)-3-(2-chloro-phen-yl)urea.1-（6-氯-1-甲基-1H-咪唑并[4,5-c]吡啶-4-基）-3-（2-氯苯基）脲
Acta Crystallogr Sect E Struct Rep Online. 2014 Jan 18;70(Pt 2):o155-6. doi: 10.1107/S1600536814000695. eCollection 2014 Feb 1.
4
3-Benzyl-6-bromo-1H-imidazo[4,5-b]pyridin-2(3H)-one.3-苄基-6-溴-1H-咪唑并[4,5-b]吡啶-2(3H)-酮
Acta Crystallogr Sect E Struct Rep Online. 2013 May 25;69(Pt 6):o962. doi: 10.1107/S1600536813013780. Print 2013 Jun 1.
5
Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation.代谢型谷氨酸受体5负变构调节剂作为体内研究的新工具。
ACS Med Chem Lett. 2012 Jul 12;3(7):544-549. doi: 10.1021/ml3000726. Epub 2012 May 22.
6
Fragile X syndrome: an update on developing treatment modalities.脆性 X 综合征：治疗方法的研究进展。
ACS Chem Neurosci. 2011 Aug 17;2(8):402-10. doi: 10.1021/cn200019z. Epub 2011 Mar 22.
7
A novel and expedient approach to new thiazoles, thiazolo[3,2-a]pyridines, dihydrothiophenes, and hydrazones incorporating thieno[2,3-b]thiophene moiety.一种合成含有噻吩并[2,3-b]噻吩部分的新型噻唑、噻唑并[3,2-a]吡啶、二氢噻吩和腙的新颖且便捷的方法。
Int J Mol Sci. 2012;13(4):5035-5047. doi: 10.3390/ijms13045035. Epub 2012 Apr 23.
8
3-Allyl-6-bromo-1H-imidazo[4,5-b]pyridin-2(3H)-one.3-烯丙基-6-溴-1H-咪唑并[4,5-b]吡啶-2(3H)-酮
Acta Crystallogr Sect E Struct Rep Online. 2011 Aug 1;67(Pt 8):o1998. doi: 10.1107/S1600536811025037. Epub 2011 Jul 9.
9
(3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu(5): Discovery of a new tool compound with activity in the OSS mouse model of addiction.mGlu(5)的(3-氰基-5-氟苯基)联芳基负变构调节剂：在成瘾的OSS小鼠模型中发现一种具有活性的新型工具化合物。
ACS Chem Neurosci. 2011 Aug 17;2(8):471-482. doi: 10.1021/cn100099n.
10
Recent advances in the design and development of novel negative allosteric modulators of mGlu(5).代谢型谷氨酸受体5（mGlu(5)）新型负变构调节剂设计与开发的最新进展
ACS Chem Neurosci. 2011 Aug 17;2(8):411-432. doi: 10.1021/cn2000266.

本文引用的文献

1
Design and synthesis of novel heterobiaryl amides as metabotropic glutamate receptor subtype 5 antagonists.新型杂联芳基酰胺作为代谢型谷氨酸受体5亚型拮抗剂的设计与合成
Bioorg Med Chem Lett. 2007 Apr 1;17(7):2074-9. doi: 10.1016/j.bmcl.2006.12.083. Epub 2007 Jan 4.
2
Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.代谢型谷氨酸受体5（mGluR5）正向变构调节剂开发中的挑战：CPPHA的发现。
Bioorg Med Chem Lett. 2007 Mar 1;17(5):1386-91. doi: 10.1016/j.bmcl.2006.11.081. Epub 2006 Dec 3.
3
Metabotropic glutamate 5 receptor antagonism is associated with antidepressant-like effects in mice.代谢型谷氨酸5受体拮抗作用与小鼠的抗抑郁样效应相关。
J Pharmacol Exp Ther. 2006 Oct;319(1):254-9. doi: 10.1124/jpet.106.103143. Epub 2006 Jun 27.
4
Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists.
Bioorg Med Chem Lett. 2006 Jul 1;16(13):3371-5. doi: 10.1016/j.bmcl.2006.04.032. Epub 2006 May 5.
5
Structure-activity relationship of thiopyrimidines as mGluR5 antagonists.硫代嘧啶作为代谢型谷氨酸受体5拮抗剂的构效关系
Bioorg Med Chem Lett. 2006 May 1;16(9):2467-9. doi: 10.1016/j.bmcl.2006.01.100. Epub 2006 Feb 14.
6
Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists.芳基甲氧基吡啶作为新型、强效且口服活性的代谢型谷氨酸受体5（mGlu5）拮抗剂。
Bioorg Med Chem Lett. 2006 Apr 1;16(7):1892-7. doi: 10.1016/j.bmcl.2005.12.088. Epub 2006 Jan 24.
7
Phenyl ureas of creatinine as mGluR5 antagonists. A structure-activity relationship study of fenobam analogues.
Bioorg Med Chem Lett. 2006 Mar 1;16(5):1142-5. doi: 10.1016/j.bmcl.2005.11.092. Epub 2005 Dec 27.
8
Therapeutic implications of the mGluR theory of fragile X mental retardation.脆性X智力障碍的代谢型谷氨酸受体理论的治疗意义
Genes Brain Behav. 2005 Aug;4(6):393-8. doi: 10.1111/j.1601-183X.2005.00135.x.
9
Suppression of two major Fragile X Syndrome mouse model phenotypes by the mGluR5 antagonist MPEP.代谢型谷氨酸受体5拮抗剂MPEP对两种主要的脆性X综合征小鼠模型表型的抑制作用
Neuropharmacology. 2005 Dec;49(7):1053-66. doi: 10.1016/j.neuropharm.2005.06.004. Epub 2005 Jul 27.
10
Catalysts for Suzuki-Miyaura coupling processes: scope and studies of the effect of ligand structure.铃木-宫浦偶联反应的催化剂：范围及配体结构影响的研究
J Am Chem Soc. 2005 Apr 6;127(13):4685-96. doi: 10.1021/ja042491j.