• 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

cis-6-oxo-hexahydro-2-oxa-1,4-diazapentalene and cis-6-oxo-hexahydropyrrolo[3,2-c]pyrazole based scaffolds: design rationale, synthesis and cysteinyl proteinase inhibition.

作者信息

Wang Yikang, Benn Alex, Flinn Nick, Monk Tracy, Ramjee Manoj, Watts John, Quibell Martin

机构信息

Amura Therapeutics Limited, Incenta House, Horizon Park, Barton Road, Comberton, Cambridge CB3 7AJ, UK.

出版信息

Bioorg Med Chem Lett. 2005 Mar 1;15(5):1327-31. doi: 10.1016/j.bmcl.2005.01.022.

DOI:10.1016/j.bmcl.2005.01.022
PMID:15713380
Abstract

The 5,5-bicycles cis-6-oxo-hexahydro-2-oxa-1,4-diazapentalene 3 and cis-6-oxo-hexahydropyrrolo[3,2-c]pyrazole 4 were designed as rotationally restricted templates towards the preparation of inhibitors of CAC1 cysteinyl proteinases. The design strategy was exemplified through the solution and solid phase preparation of potent inhibitors of human cathepsin K and may potentially be applied to inhibitors of other CAC1 proteinases.

摘要

相似文献

1
cis-6-oxo-hexahydro-2-oxa-1,4-diazapentalene and cis-6-oxo-hexahydropyrrolo[3,2-c]pyrazole based scaffolds: design rationale, synthesis and cysteinyl proteinase inhibition.
Bioorg Med Chem Lett. 2005 Mar 1;15(5):1327-31. doi: 10.1016/j.bmcl.2005.01.022.
2
Synthesis and evaluation of cis-hexahydropyrrolo[3,2-b]pyrrol-3-one peptidomimetic inhibitors of CAC1 cysteinyl proteinases.CAC1半胱氨酸蛋白酶的顺式六氢吡咯并[3,2 - b]吡咯 - 3 - 酮拟肽抑制剂的合成与评价
Bioorg Med Chem. 2005 Feb 1;13(3):609-25. doi: 10.1016/j.bmc.2004.10.060.
3
Arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 2: Optimization of P1 and N-aryl.芳氨基乙酰胺作为组织蛋白酶S的非共价抑制剂。第2部分：P1和N-芳基的优化
Bioorg Med Chem Lett. 2006 Mar 15;16(6):1486-90. doi: 10.1016/j.bmcl.2005.12.056. Epub 2006 Jan 18.
4
Conformationally constrained 1,3-diamino ketones: a series of potent inhibitors of the cysteine protease cathepsin K.构象受限的1,3-二氨基酮：一系列半胱氨酸蛋白酶组织蛋白酶K的强效抑制剂。
J Med Chem. 1998 Sep 10;41(19):3563-7. doi: 10.1021/jm980295f.
5
Benzodioxocin-3-ones and N-acyl-3-amino-3-buten-2-ones: novel classes of cathepsin K cysteine protease inhibitors.苯并二氧杂环己酮-3-酮和N-酰基-3-氨基-3-丁烯-2-酮：新型组织蛋白酶K半胱氨酸蛋白酶抑制剂。
J Pept Res. 2004 Mar;63(3):265-9. doi: 10.1111/j.1399-3011.2004.00138.x.
6
Structure-based design of cathepsin K inhibitors containing a benzyloxy-substituted benzoyl peptidomimetic.含苄氧基取代苯甲酰拟肽的组织蛋白酶K抑制剂的基于结构的设计
J Med Chem. 1998 Oct 8;41(21):3923-7. doi: 10.1021/jm980474x.
7
3,4-disubstituted azetidinones as selective inhibitors of the cysteine protease cathepsin K. Exploring P3 elements for potency and selectivity.3,4-二取代氮杂环丁烷酮作为半胱氨酸蛋白酶组织蛋白酶K的选择性抑制剂。探索用于提高效力和选择性的P3元件。
Bioorg Med Chem Lett. 2005 Mar 1;15(5):1529-34. doi: 10.1016/j.bmcl.2004.12.088.
8
The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors.一类新型3,4-二芳基吡唑类Hsp90抑制剂的鉴定、合成、蛋白质晶体结构及体外生化评价
Bioorg Med Chem Lett. 2005 Jul 15;15(14):3338-43. doi: 10.1016/j.bmcl.2005.05.046.
9
Design and synthesis of protein-protein interaction mimics as Plasmodium falciparum cysteine protease, falcipain-2 inhibitors.设计和合成蛋白-蛋白相互作用模拟物作为恶性疟原虫半胱氨酸蛋白酶、falcipain-2 的抑制剂。
Eur J Med Chem. 2011 Jun;46(6):2083-90. doi: 10.1016/j.ejmech.2011.02.061. Epub 2011 Mar 3.
10
Functionalised 2,3-dimethyl-3-aminotetrahydrofuran-4-one and N-(3-oxo-hexahydrocyclopenta[b]furan-3a-yl)acylamide based scaffolds: synthesis and cysteinyl proteinase inhibition.基于功能化的2,3-二甲基-3-氨基四氢呋喃-4-酮和N-(3-氧代-六氢环戊并[b]呋喃-3a-基)酰胺的支架：合成与半胱氨酸蛋白酶抑制作用
Bioorg Med Chem. 2004 Jun 1;12(11):2903-25. doi: 10.1016/j.bmc.2004.03.042.

引用本文的文献

1
Covalent Tethers for Precise Amino Alcohol Syntheses: Ring Opening of Epoxides by Pendant Sulfamates and Sulfamides.共价键连接用于精确的氨基酸醇合成：通过悬垂的磺酸盐和磺酰胺开环环氧化物。
Org Lett. 2023 Feb 17;25(6):982-986. doi: 10.1021/acs.orglett.3c00053. Epub 2023 Feb 6.
2
Cathepsin K inhibitors for osteoporosis and potential off-target effects.组织蛋白酶 K 抑制剂治疗骨质疏松症及其潜在的非靶标作用。
Expert Opin Investig Drugs. 2009 May;18(5):585-600. doi: 10.1517/13543780902832661.