• 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

Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179).

作者信息

Einsiedel J, Hübner H, Gmeiner P

机构信息

Department of Medicinal Chemistry, Emil Fischer Center, Friedrich-Alexander University, Schuhstrasse 19, D-91052, Erlangen, Germany.

出版信息

Bioorg Med Chem Lett. 2001 Sep 17;11(18):2533-6. doi: 10.1016/s0960-894x(01)00484-x.

DOI:10.1016/s0960-894x(01)00484-x
PMID:11549463
Abstract

Conformationally restricted benzamide bioisosteres were investigated when the chiral phenyldihydroimidazole derivative 4e (FAUC 179) showed strong and highly selective dopamine D4 receptor binding (K(i)high=0.95nM). Mitogenesis experiments indicated partial agonist properties (42%). EPC syntheses of the target compounds of type 4 were performed starting from alpha-amino acids.

摘要

相似文献

1
Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179).
Bioorg Med Chem Lett. 2001 Sep 17;11(18):2533-6. doi: 10.1016/s0960-894x(01)00484-x.
2
Cyclic amidines as benzamide bioisosteres: EPC synthesis and SAR studies leading to the selective dopamine D4 receptor agonist FAUC 312.
Bioorg Med Chem Lett. 2003 Mar 10;13(5):851-4. doi: 10.1016/s0960-894x(03)00004-0.
3
Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213).基于理性的选择性多巴胺D4受体配体的效能调节，得到完全拮抗剂2-[4-(4-氯苯基)哌嗪-1-基甲基]吡唑并[1,5-a]吡啶（曲线下面积213）。
J Med Chem. 2001 Aug 16;44(17):2691-4. doi: 10.1021/jm015522j.
4
The agonist activities of the putative antipsychotic agents, L-745,870 and U-101958 in HEK293 cells expressing the human dopamine D4.4 receptor.假定抗精神病药物L-745,870和U-101958在表达人多巴胺D4.4受体的HEK293细胞中的激动剂活性。
Br J Pharmacol. 1998 Jul;124(5):889-96. doi: 10.1038/sj.bjp.0701921.
5
Cyanoindole derivatives as highly selective dopamine D(4) receptor partial agonists: solid-phase synthesis, binding assays, and functional experiments.
J Med Chem. 2000 Nov 16;43(23):4563-9. doi: 10.1021/jm0009989.
6
Aplindore (DAB-452), a high affinity selective dopamine D2 receptor partial agonist.阿普林多（DAB - 452），一种高亲和力的选择性多巴胺D2受体部分激动剂。
Eur J Pharmacol. 2006 Dec 15;552(1-3):36-45. doi: 10.1016/j.ejphar.2006.08.063. Epub 2006 Sep 14.
7
Phenylpiperazinylmethylindolecarboxylates and derivatives as selective D(4)-ligands.苯基哌嗪基甲基吲哚羧酸盐及其衍生物作为选择性D(4)配体。
Bioorg Med Chem. 2002 Jun;10(6):1671-9. doi: 10.1016/s0968-0896(02)00042-1.
8
2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356.
Bioorg Med Chem Lett. 2002 Aug 5;12(15):1937-40. doi: 10.1016/s0960-894x(02)00316-5.
9
2,2-Dicyanovinyl as a nonaromatic aryl bioisostere: synthesis, binding experiments and SAR studies of highly selective dopamine D4 receptor ligands.
Bioorg Med Chem Lett. 1999 Jul 19;9(14):1969-72. doi: 10.1016/s0960-894x(99)00302-9.
10
(Aryloxy)alkylamines as selective human dopamine D4 receptor antagonists: potential antipsychotic agents.（芳氧基）烷基胺作为选择性人多巴胺D4受体拮抗剂：潜在的抗精神病药物。
J Med Chem. 1997 Dec 5;40(25):4026-9. doi: 10.1021/jm970422s.

引用本文的文献

1
Dopamine Receptor Ligand Selectivity-An In Silico/In Vitro Insight.多巴胺受体配体选择性——计算机模拟/体外研究洞察
Biomedicines. 2023 May 17;11(5):1468. doi: 10.3390/biomedicines11051468.
2
Copper-catalyzed diamination of unactivated alkenes with hydroxylamines.铜催化未活化烯烃与羟胺的双胺化反应。
Chem Sci. 2015 Jul 1;6(7):4279-4283. doi: 10.1039/c5sc00897b. Epub 2015 May 18.
3
Efficient microwave assisted synthesis of optically active bicyclic 2-pyridinones via delta2-thiazolines.通过δ2-噻唑啉高效微波辅助合成光学活性双环2-吡啶酮
Mol Divers. 2003;7(2-4):165-9. doi: 10.1023/b:modi.0000006800.46154.99.