• 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

二肽基肽酶IV的(3R,4S)-4-(2,4,5-三氟苯基)吡咯烷-3-基胺抑制剂：合成、体外、体内及X射线晶体学表征

(3R,4S)-4-(2,4,5-Trifluorophenyl)-pyrrolidin-3-ylamine inhibitors of dipeptidyl peptidase IV: synthesis, in vitro, in vivo, and X-ray crystallographic characterization.

作者信息

Wright Stephen W, Ammirati Mark J, Andrews Kim M, Brodeur Anne M, Danley Dennis E, Doran Shawn D, Lillquist Jay S, Liu Shenping, McClure Lester D, McPherson R Kirk, Olson Thanh V, Orena Stephen J, Parker Janice C, Rocke Benjamin N, Soeller Walter C, Soglia Carolyn B, Treadway Judith L, Vanvolkenburg Maria A, Zhao Zhengrong, Cox Eric D

机构信息

Pfizer Global Research and Development, Cardiovascular and Metabolic Diseases, MS 8220-3141, Eastern Point Road, Groton, CT 06340, USA.

出版信息

Bioorg Med Chem Lett. 2007 Oct 15;17(20):5638-42. doi: 10.1016/j.bmcl.2007.07.081. Epub 2007 Aug 22.

DOI:10.1016/j.bmcl.2007.07.081
PMID:17822893
Abstract

A series of pyrrolidine based inhibitors of dipeptidyl peptidase IV were developed from a high throughput screening hit for the treatment of type 2 diabetes. Potency, selectivity, and pharmacokinetic properties were optimized resulting in the identification of a pre-clinical candidate for further profiling.

摘要

从用于治疗2型糖尿病的高通量筛选命中物出发，开发了一系列基于吡咯烷的二肽基肽酶IV抑制剂。对效力、选择性和药代动力学性质进行了优化，从而鉴定出一个用于进一步分析的临床前候选物。

相似文献

1
(3R,4S)-4-(2,4,5-Trifluorophenyl)-pyrrolidin-3-ylamine inhibitors of dipeptidyl peptidase IV: synthesis, in vitro, in vivo, and X-ray crystallographic characterization.二肽基肽酶IV的(3R,4S)-4-(2,4,5-三氟苯基)吡咯烷-3-基胺抑制剂：合成、体外、体内及X射线晶体学表征
Bioorg Med Chem Lett. 2007 Oct 15;17(20):5638-42. doi: 10.1016/j.bmcl.2007.07.081. Epub 2007 Aug 22.
2
Synthesis and structure-activity relationships of potent 4-fluoro-2-cyanopyrrolidine dipeptidyl peptidase IV inhibitors.强效4-氟-2-氰基吡咯烷二肽基肽酶IV抑制剂的合成及其构效关系
Bioorg Med Chem. 2008 Apr 1;16(7):4093-106. doi: 10.1016/j.bmc.2008.01.016. Epub 2008 Jan 16.
3
From lead to preclinical candidate: optimization of beta-homophenylalanine based inhibitors of dipeptidyl peptidase IV.从先导化合物到临床前候选药物：基于β-高苯丙氨酸的二肽基肽酶IV抑制剂的优化
Bioorg Med Chem Lett. 2009 Aug 15;19(16):4818-23. doi: 10.1016/j.bmcl.2009.06.036. Epub 2009 Jun 13.
4
Discovery, structure-activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors.(5-取代-吡咯烷基-2-羰基)-2-氰基吡咯烷作为强效二肽基肽酶IV抑制剂的发现、构效关系及药理评价
J Med Chem. 2006 Jun 15;49(12):3520-35. doi: 10.1021/jm051283e.
5
cis-2,5-dicyanopyrrolidine inhibitors of dipeptidyl peptidase IV: synthesis and in vitro, in vivo, and X-ray crystallographic characterization.二肽基肽酶IV的顺式-2,5-二氰基吡咯烷抑制剂：合成及体外、体内和X射线晶体学表征
J Med Chem. 2006 Jun 1;49(11):3068-76. doi: 10.1021/jm0600085.
6
Diastereoselective synthesis and configuration-dependent activity of (3-substituted-cycloalkyl)glycine pyrrolidides and thiazolidides as dipeptidyl peptidase IV inhibitors.（3-取代环烷基）甘氨酸吡咯烷酰胺和噻唑烷酰胺作为二肽基肽酶IV抑制剂的非对映选择性合成及构型依赖性活性
Bioorg Med Chem Lett. 2004 Feb 23;14(4):859-63. doi: 10.1016/j.bmcl.2003.12.013.
7
Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors.取代的吡咯烷-2,4-二羧酸酰胺作为有效的二肽基肽酶IV抑制剂。
Bioorg Med Chem Lett. 2006 Jun 15;16(12):3268-72. doi: 10.1016/j.bmcl.2006.03.037. Epub 2006 Apr 11.
8
Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors.基于三唑并哌嗪的β-氨基酰胺作为强效口服活性二肽基肽酶IV（DPP-4）抑制剂的设计、合成及生物学评价
Bioorg Med Chem Lett. 2007 Nov 1;17(21):5934-9. doi: 10.1016/j.bmcl.2007.07.100. Epub 2007 Aug 23.
9
(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.(3R)-4-[(3R)-3-氨基-4-(2,4,5-三氟苯基)丁酰基]-3-(2,2,2-三氟乙基)-1,4-二氮杂环庚烷-2-酮，一种用于治疗2型糖尿病的选择性二肽基肽酶IV抑制剂。
Bioorg Med Chem Lett. 2007 Jan 1;17(1):49-52. doi: 10.1016/j.bmcl.2006.09.099. Epub 2006 Oct 5.
10
Design and synthesis of new potent dipeptidyl peptidase IV inhibitors with enhanced ex vivo duration.
Bioorg Med Chem. 2007 Apr 1;15(7):2631-50. doi: 10.1016/j.bmc.2007.01.041. Epub 2007 Jan 26.

引用本文的文献

1
Comprehensive analysis of the Co-structures of dipeptidyl peptidase IV and its inhibitor.二肽基肽酶IV与其抑制剂的共结构综合分析。
BMC Struct Biol. 2016 Aug 5;16:11. doi: 10.1186/s12900-016-0062-8.