• 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

Sugar-substituted 2-azetidinone cholesterol absorption inhibitors: enhanced potency by modification of the sugar.

作者信息

Vaccaro W D, Davis H R

机构信息

Schering-Plough Research Institute, Kenilworth, New Jersey 07033-0539, USA.

出版信息

Bioorg Med Chem Lett. 1998 Feb 3;8(3):313-8. doi: 10.1016/s0960-894x(98)00008-0.

DOI:10.1016/s0960-894x(98)00008-0
PMID:9871676
Abstract

A glucuronide conjugate of the potent 2-azetidinone cholesterol absorption inhibitor Sch 58235 was synthesized to confirm the structure of a metabolite isolated from in vivo sources. A series of 2-azetidinone glycosides was prepared via Schmidt trichloroimidate methodology. Enhanced cholesterol absorption inhibition was achieved by modification of the sugar moiety.

摘要

相似文献

1
Sugar-substituted 2-azetidinone cholesterol absorption inhibitors: enhanced potency by modification of the sugar.
Bioorg Med Chem Lett. 1998 Feb 3;8(3):313-8. doi: 10.1016/s0960-894x(98)00008-0.
2
Sugar-substituted 2-azetidinones as cholesterol absorption inhibitors.作为胆固醇吸收抑制剂的糖取代氮杂环丁烷-2-酮
Bioorg Med Chem Lett. 1998 Jan 6;8(1):35-40. doi: 10.1016/s0960-894x(97)10185-8.
3
2-Azetidinone cholesterol absorption inhibitors: increased potency by substitution of the C-4 phenyl ring.2-氮杂环丁烷酮胆固醇吸收抑制剂:通过C-4苯环取代提高活性。
Bioorg Med Chem. 1998 Sep;6(9):1429-37. doi: 10.1016/s0968-0896(98)00073-x.
4
Carboxy-substituted 2-azetidinones as cholesterol absorption inhibitors.作为胆固醇吸收抑制剂的羧基取代的2-氮杂环丁酮
Bioorg Med Chem Lett. 1998 Feb 3;8(3):319-22. doi: 10.1016/s0960-894x(98)00009-2.
5
Discovery of 1-(4-fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)-hydroxypropyl]-(4S)-(4 -hydroxyphenyl)-2-azetidinone (SCH 58235): a designed, potent, orally active inhibitor of cholesterol absorption.1-(4-氟苯基)-(3R)-[3-(4-氟苯基)-(3S)-羟丙基]-(4S)-(4-羟苯基)-2-氮杂环丁酮(SCH 58235)的发现:一种设计合成的强效口服活性胆固醇吸收抑制剂。
J Med Chem. 1998 Mar 12;41(6):973-80. doi: 10.1021/jm970701f.
6
Synthesis of iodinated biochemical tools related to the 2-azetidinone class of cholesterol absorption inhibitors.与2-氮杂环丁酮类胆固醇吸收抑制剂相关的碘化生化工具的合成。
Bioorg Med Chem Lett. 2002 Feb 11;12(3):311-4. doi: 10.1016/s0960-894x(01)00750-8.
7
2-Azetidinone cholesterol absorption inhibitors: structure-activity relationships on the heterocyclic nucleus.
J Med Chem. 1996 Sep 13;39(19):3684-93. doi: 10.1021/jm960405n.
8
Synthesis of fluorescent biochemical tools related to the 2-azetidinone class of cholesterol absorption inhibitors.与2-氮杂环丁酮类胆固醇吸收抑制剂相关的荧光生化工具的合成。
Bioorg Med Chem Lett. 2002 Feb 11;12(3):315-8. doi: 10.1016/s0960-894x(01)00752-1.
9
Substituted 2-azaspiro[5.3]nonan-1-ones as potent cholesterol absorption inhibitors: defining a binding conformation for SCH 48461.取代的2-氮杂螺[5.3]壬烷-1-酮作为有效的胆固醇吸收抑制剂:确定SCH 48461的结合构象。
J Med Chem. 1995 Dec 8;38(25):4875-7. doi: 10.1021/jm00025a002.
10
Synthesis of a biotin-tagged photoaffinity probe of 2-azetidinone cholesterol absorption inhibitors.2-氮杂环丁烷酮胆固醇吸收抑制剂的生物素标记光亲和探针的合成。
Bioorg Med Chem. 2003 Apr 17;11(8):1639-42. doi: 10.1016/s0968-0896(03)00047-6.

引用本文的文献

1
Expanding the Chemical Space of Electrophilic β-Glycosyl β-Lactams through Photoinduced Diastereoselective Functionalization.通过光诱导非对映选择性官能团化扩展亲电β-糖基β-内酰胺的化学空间
Org Lett. 2024 Jul 5;26(26):5500-5505. doi: 10.1021/acs.orglett.4c01844. Epub 2024 Jun 20.
2
Synthesis and Modeling of Ezetimibe Analogues.依泽替米贝类似物的合成与建模。
Molecules. 2021 May 22;26(11):3107. doi: 10.3390/molecules26113107.
3
Chemoenzymatic Approach toward the Synthesis of 3--(α/β)-Glucosylated 3-Hydroxy-β-lactams.化学酶法合成3-(α/β)-葡萄糖基化3-羟基-β-内酰胺
ACS Omega. 2018 Nov 30;3(11):15235-15245. doi: 10.1021/acsomega.8b01969. Epub 2018 Nov 12.
4
Anomeric modification of carbohydrates using the Mitsunobu reaction.利用光延反应对碳水化合物进行端基异构修饰。
Beilstein J Org Chem. 2018 Jun 29;14:1619-1636. doi: 10.3762/bjoc.14.138. eCollection 2018.
5
(2RS,3SR,10SR,11RS)-3,10-Diphen-oxy-18,21-dioxa-5,8-diaza-penta-cyclo-[20.4.0.0.0.0]hexa-cosa-1(26),12,14,16,22,24-hexa-ene-4,9-dione ethyl acetate hemisolvate.(2RS,3SR,10SR,11RS)-3,10-二苯氧基-18,21-二氧杂-5,8-二氮杂-五环-[20.4.0.0².⁶.0³.⁵.0⁹.¹¹]二十六碳-1(26),12,14,16,22,24-六烯-4,9-二酮乙酸乙酯半溶剂化物
Acta Crystallogr Sect E Struct Rep Online. 2011 Aug 1;67(Pt 8):o2203. doi: 10.1107/S1600536811030200. Epub 2011 Jul 30.
6
Ethyl 1-(4-chloro-phen-yl)-3-[1-(4-meth-oxy-phen-yl)-4-oxo-3-phenyl-azetidin-2-yl]-2-nitro-2,3,10,10a-tetra-hydro-1H,5H-pyr-rolo[1,2-b]isoquinoline-10a-carboxyl-ate.1-(4-氯苯基)-3-[1-(4-甲氧基苯基)-4-氧代-3-苯基氮杂环丁烷-2-基]-2-硝基-2,3,10,10a-四氢-1H,5H-吡咯并[1,2-b]异喹啉-10a-羧酸乙酯
Acta Crystallogr Sect E Struct Rep Online. 2008 Sep 30;64(Pt 10):o2042. doi: 10.1107/S1600536808030961.