• 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

1,2,3,4,5,6-六氢-1,6-亚甲基-2-苯并氮杂卓的合成及药理性质

Synthesis and pharmacological properties of 1,2,3,4,5,6-hexahydro-1,6-methano-2-benzazocines.

作者信息

Mazzocchi P H, Stahly B C

出版信息

J Med Chem. 1981 Apr;24(4):457-62. doi: 10.1021/jm00136a016.

DOI:10.1021/jm00136a016
PMID:7265131
Abstract

1,2,3,4,5,6-Hexahydro-1,6-methano-2-benzazocine, 2'-methoxy-1,2,3,4,5,6-hexahydro-1,6-methano-2-benzazocine, and N-alkyl derivatives of 2'-hydroxy-1,2,3,4,5,6-hexahydro-1,6-methano-2-benzazocine have been synthesized in order to evaluate their analgesic activities. These compounds show only slight antinociceptive activities in the mouse hot-plate assay.

摘要

为评估其镇痛活性,已合成了1,2,3,4,5,6-六氢-1,6-亚甲基-2-苯并氮杂卓、2'-甲氧基-1,2,3,4,5,6-六氢-1,6-亚甲基-2-苯并氮杂卓以及2'-羟基-1,2,3,4,5,6-六氢-1,6-亚甲基-2-苯并氮杂卓的N-烷基衍生物。这些化合物在小鼠热板试验中仅表现出轻微的抗伤害感受活性。

相似文献

1
Synthesis and pharmacological properties of 1,2,3,4,5,6-hexahydro-1,6-methano-2-benzazocines.1,2,3,4,5,6-六氢-1,6-亚甲基-2-苯并氮杂卓的合成及药理性质
J Med Chem. 1981 Apr;24(4):457-62. doi: 10.1021/jm00136a016.
2
Synthesis, stereochemistry, and analgesic activity of 4-mono- and 4,4-disubstituted 1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines.4-单取代和4,4-二取代的1,2,3,4,5,6-六氢-2,6-亚甲基-3-苯并氮杂卓的合成、立体化学及镇痛活性
J Med Chem. 1985 Feb;28(2):177-81. doi: 10.1021/jm00380a005.
3
Synthesis and pharmacology of 8-amino-3-(cyclopropylmethyl)-1,2,3,4,5,6-hexahydro-cis-6,11-dimethyl-2,6-methano-3-benzazocine and related compounds.
J Med Chem. 1980 Jan;23(1):71-4. doi: 10.1021/jm00175a013.
4
9-hydroxy-1,2,3,4,5,6-hexahydro-1,5-methano-3-benzazocine derivatives as analgesics.9-羟基-1,2,3,4,5,6-六氢-1,5-亚甲基-3-苯并氮杂卓衍生物作为镇痛药。
J Med Chem. 1977 Feb;20(2):310-2. doi: 10.1021/jm00212a027.
5
Novel nonnarcotic analgesics with an improved therapeutic ratio. Structure-activity relationships of 8-(methylthio)- and 8-(acylthio)-1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines.具有改善治疗指数的新型非麻醉性镇痛药。8-(甲硫基)-和8-(酰硫基)-1,2,3,4,5,6-六氢-2,6-亚甲基-3-苯并氮杂卓的构效关系。
J Med Chem. 1985 Nov;28(11):1656-61. doi: 10.1021/jm00149a020.
6
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 7: syntheses and opioid receptor properties of cyclic variants of cyclazocine.重新定义2,6-亚甲基-3-苯并氮杂卓的构效关系。第7部分:环唑辛环类似物的合成及阿片受体性质
Bioorg Med Chem Lett. 2009 Jan 15;19(2):365-8. doi: 10.1016/j.bmcl.2008.11.076. Epub 2008 Nov 24.
7
Synthesis and analgetic activity of some benzomorphan analogues.
J Med Chem. 1978 Nov;21(11):1105-10. doi: 10.1021/jm00209a003.
8
Synthesis and analgetic activity of 1,2,3,4,5,6-hexahydro-1,6-methano-3-benzozocines.
J Med Chem. 1978 Feb;21(2):238-40. doi: 10.1021/jm00200a021.
9
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 4. Opioid receptor binding properties of 8-[N-(4'-phenyl)-phenethyl)carboxamido] analogues of cyclazocine and ethylketocycalzocine.重新定义2,6-亚甲基-3-苯并氮杂䓬的构效关系。4. 环唑辛和乙基酮环唑辛的8-[N-(4'-苯基)-苯乙基]甲酰胺类似物的阿片受体结合特性。
J Med Chem. 2006 Sep 7;49(18):5635-9. doi: 10.1021/jm060278n.
10
Antinociceptive activity of intracisternally and intrathecally administered eptazocine, a novel analgesic, in mice.
Methods Find Exp Clin Pharmacol. 1990 Jan-Feb;12(1):11-5.

引用本文的文献

1
Evolution of a strategy for preparing bioactive small molecules by sequential multicomponent assembly processes, cyclizations, and diversification.通过顺序多组分组装过程、环化反应和多样化反应制备生物活性小分子的策略的演变。
Org Biomol Chem. 2014 Oct 21;12(39):7659-72. doi: 10.1039/c4ob00835a. Epub 2014 Aug 19.
2
Facile Syntheses of Substituted, Conformationally-Constrained Benzoxazocines and Benzazocines via Sequential Multicomponent Assembly and Cyclization.通过顺序多组分组装和环化反应简便合成取代的、构象受限的苯并恶唑嗪和苯并氮杂环辛烷。
Tetrahedron Lett. 2011 Dec 21;52(51):6855-6858. doi: 10.1016/j.tetlet.2011.10.022.