• 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

作为抗糖尿病药物的吡咯烷和哌啶磺酰胺衍生物的设计与合成

Design and synthesis of sulfonamide derivatives of pyrrolidine and piperidine as anti-diabetic agents.

作者信息

Sharma Radhika, Soman Shubhangi S

机构信息

Department of Chemistry, Faculty of Science, The M. S. University of Baroda, Vadodara, Gujarat 390 002, India.

Department of Chemistry, Faculty of Science, The M. S. University of Baroda, Vadodara, Gujarat 390 002, India.

出版信息

Eur J Med Chem. 2015 Jan 27;90:342-50. doi: 10.1016/j.ejmech.2014.11.041. Epub 2014 Nov 22.

DOI:10.1016/j.ejmech.2014.11.041
PMID:25437620
Abstract

Type 2 diabetes (T2D) is a lifestyle disease affecting millions of people worldwide. Various therapies are available for the management of T2D and dipeptidyl peptidase-IV (DPP-IV) inhibition has emerged as a promising therapy for the treatment of type 2 diabetes (T2D). Here we report design, synthesis and in vitro efficacy of sulfonamide derivatives of pyrrolidine and piperidine as anti-diabetic agents. Amongst all the compounds synthesized in this series, 9a, is the most potent (IC50 = 41.17 nM).

摘要

2型糖尿病(T2D)是一种影响全球数百万人的生活方式疾病。有多种疗法可用于管理T2D,而二肽基肽酶-IV(DPP-IV)抑制已成为治疗2型糖尿病(T2D)的一种有前景的疗法。在此,我们报告吡咯烷和哌啶的磺酰胺衍生物作为抗糖尿病药物的设计、合成及体外疗效。在该系列合成的所有化合物中,9a最为有效(IC50 = 41.17 nM)。

相似文献

1
Design and synthesis of sulfonamide derivatives of pyrrolidine and piperidine as anti-diabetic agents.作为抗糖尿病药物的吡咯烷和哌啶磺酰胺衍生物的设计与合成
Eur J Med Chem. 2015 Jan 27;90:342-50. doi: 10.1016/j.ejmech.2014.11.041. Epub 2014 Nov 22.
2
Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.吡咯烷-2-甲腈和 4-氟吡咯烷-2-甲腈衍生物的合成及作为二肽基肽酶-4 抑制剂用于治疗 2 型糖尿病的生物评价。
Bioorg Med Chem. 2013 Dec 1;21(23):7418-29. doi: 10.1016/j.bmc.2013.09.048. Epub 2013 Oct 1.
3
Rational design and synthesis of new tetralin-sulfonamide derivatives as potent anti-diabetics and DPP-4 inhibitors: 2D & 3D QSAR, in vivo radiolabeling and bio distribution studies.新型四氢萘-磺酰胺衍生物的合理设计与合成及其作为强效抗糖尿病和 DPP-4 抑制剂的研究:2D 和 3D QSAR、体内放射性标记和生物分布研究。
Bioorg Chem. 2018 Dec;81:481-493. doi: 10.1016/j.bioorg.2018.09.021. Epub 2018 Sep 12.
4
Synthesis, evaluation and molecular docking of prolyl-fluoropyrrolidine derivatives as dipeptidyl peptidase IV inhibitors.脯氨酰-氟代吡咯烷衍生物的合成、评价及作为二肽基肽酶 IV 抑制剂的分子对接。
Chem Biol Drug Des. 2013 Aug;82(2):156-66. doi: 10.1111/cbdd.12142. Epub 2013 Jun 29.
5
Design, synthesis, biological screening, and molecular docking studies of piperazine-derived constrained inhibitors of DPP-IV for the treatment of type 2 diabetes.用于治疗2型糖尿病的哌嗪衍生的DPP-IV受限抑制剂的设计、合成、生物学筛选及分子对接研究
Chem Biol Drug Des. 2015 Apr;85(4):439-46. doi: 10.1111/cbdd.12426. Epub 2014 Oct 16.
6
Synthesis of piperazine sulfonamide analogs as diabetic-II inhibitors and their molecular docking study.哌嗪磺酰胺类似物作为糖尿病-II 抑制剂的合成及其分子对接研究。
Eur J Med Chem. 2017 Dec 1;141:530-537. doi: 10.1016/j.ejmech.2017.10.028. Epub 2017 Oct 12.
7
Novel N-substituted 4-hydrazino piperidine derivative as a dipeptidyl peptidase IV inhibitor.新型N-取代4-肼基哌啶衍生物作为二肽基肽酶IV抑制剂
Bioorg Med Chem Lett. 2009 Sep 1;19(17):5021-5. doi: 10.1016/j.bmcl.2009.07.058. Epub 2009 Jul 12.
8
Synthesis and biological evaluation of novel pyrrolidine acid analogs as potent dual PPARα/γ agonists.新型吡咯烷酸类似物作为强效双PPARα/γ激动剂的合成与生物学评价
Bioorg Med Chem Lett. 2015 Mar 15;25(6):1196-205. doi: 10.1016/j.bmcl.2015.01.066. Epub 2015 Feb 4.
9
Synthesis and evaluation of camphor and cytisine-based cyanopyrrolidines as DPP-IV inhibitors for the treatment of type 2 diabetes mellitus.合成与评价基于莰酮和野靛碱的氰基吡咯烷类化合物作为 DPP-IV 抑制剂用于治疗 2 型糖尿病。
Bioorg Med Chem. 2018 Aug 15;26(15):4402-4409. doi: 10.1016/j.bmc.2018.07.018. Epub 2018 Jul 11.
10
Design, synthesis, biological evaluation, and docking studies of (s)-phenylalanine derivatives with a 2-cyanopyrrolidine moiety as potent dipeptidyl peptidase 4 inhibitors.设计、合成、生物评价及含 2-氰基吡咯烷部分的(S)-苯丙氨酸衍生物作为强效二肽基肽酶 4 抑制剂的对接研究。
Chem Biol Drug Des. 2013 Aug;82(2):140-6. doi: 10.1111/cbdd.12139. Epub 2013 Jun 29.

引用本文的文献

1
Dipeptidyl Peptidase-4 Inhibitors: A Systematic Review of Structure-Activity Relationship Studies.二肽基肽酶-4抑制剂:结构-活性关系研究的系统综述
Iran J Pharm Res. 2024 Oct 29;23(1):e151581. doi: 10.5812/ijpr-151581. eCollection 2024 Jan-Dec.
2
Design and Synthesis of 1-(4-Bromo-2-(Pyrrolidine-1-Yl) Benzyl) Piperidine-based Derivatives as Anti-tubulin Agents.基于1-(4-溴-2-(吡咯烷-1-基)苄基)哌啶的抗微管蛋白剂衍生物的设计与合成
Curr Top Med Chem. 2025;25(11):1389-1402. doi: 10.2174/0115680266336578241114072129.
3
Morpholine, Piperazine, and Piperidine Derivatives as Antidiabetic Agents.
吗啡啉、哌嗪和哌啶衍生物作为抗糖尿病药物。
Molecules. 2024 Jun 26;29(13):3043. doi: 10.3390/molecules29133043.
4
Integration of Deep Learning and Sequential Metabolism to Rapidly Screen Dipeptidyl Peptidase (DPP)-IV Inhibitors from .深度学习与序列代谢相结合,快速筛选二肽基肽酶 (DPP)-IV 抑制剂。
Molecules. 2023 Nov 1;28(21):7381. doi: 10.3390/molecules28217381.
5
New quinoxaline compounds as DPP-4 inhibitors and hypoglycemics: design, synthesis, computational and bio-distribution studies.新型喹喔啉化合物作为二肽基肽酶-4抑制剂和降血糖药物:设计、合成、计算及生物分布研究
RSC Adv. 2021 Nov 17;11(58):36989-37010. doi: 10.1039/d1ra06799k. eCollection 2021 Nov 10.
6
Synthesis, spectral characterization, docking studies and biological activity of urea, thiourea, sulfonamide and carbamate derivatives of imatinib intermediate.伊马替尼中间体的脲、硫脲、磺胺和氨基甲酸酯衍生物的合成、光谱表征、对接研究和生物活性。
Mol Divers. 2019 Aug;23(3):723-738. doi: 10.1007/s11030-018-9906-4. Epub 2018 Dec 17.
7
Crystal structure of 15-(2-chloro-phen-yl)-6b-hy-droxy-17-methyl-6b,7,16,17-tetra-hydro-7,14a-methanona-phtho[1',8':1,2,3]pyrrolo-[3',2':8,8a]azuleno[5,6-b]quinolin-14(15H)-one.15-(2-氯苯基)-6b-羟基-17-甲基-6b,7,16,17-四氢-7,14a-亚甲基萘并[1',8':1,2,3]吡咯并[3',2':8,8a]薁并[5,6-b]喹啉-14(15H)-酮的晶体结构
Acta Crystallogr E Crystallogr Commun. 2015 Dec 31;71(Pt 12):o1091-2. doi: 10.1107/S2056989015024767. eCollection 2015 Dec 1.