Design, Synthesis, and Pharmacological Evaluation of Highly Potent and Selective Dipeptidyl Peptidase-4 Inhibitors
文献类型：期刊论文
| 作者 | Jiang, Tao; Zhou, Yuren; Zhu, Jianming; Chen, Zhuxi; Sun, Peng; Zhang, Qiang; Wang, Zhen ; Shao, Qiang; Jiang, Xiangrui; Li, Bo
|
| 刊名 | ARCHIV DER PHARMAZIE
 |
| 出版日期 | 2015-06 |
| 卷号 | 348期号:6页码:399-407 |
| 关键词 | beta-Homophenylalanine DPP-4 Drug design Inhibitors P2-binding moiety |
| ISSN号 | 0365-6233 |
| DOI | 10.1002/ardp.201500082 |
| 文献子类 | Article |
| 英文摘要 | The optimization of a series of fused -homophenylalanine inhibitors of dipeptidyl peptidase-4 (DPP-4) is described. Modification on the P2-binding moiety of 6 (IC50=10nM) led to the discovery of -homophenylalanine derivatives containing pyrrolidin-2-ylmethyl amides. The introduction of a sulfamine in the meta position of the phenyl ring improved the potency against DPP-4 (6-12-fold increase). Compound 14k showed DPP-4 inhibitory activity with an IC50 value of 0.87nM. Meanwhile, in vivo experiments exhibited that 14h had an efficiency comparable to sitagliptin at the dose of 10mg/kg. |
| WOS关键词 | IV INHIBITOR ; DISCOVERY |
| 资助项目 | National Natural Science Foundation of China[21373258] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000355625200003 |
| 出版者 | WILEY-V C H VERLAG GMBH |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276511]  |
| 专题 | 药物化学研究室 药物发现与设计中心 药理学第三研究室 |
| 通讯作者 | Jiang, Xiangrui |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, Key Lab Receptor Res, Drug Discovery & Design Ctr, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Jiang, Tao,Zhou, Yuren,Zhu, Jianming,et al. Design, Synthesis, and Pharmacological Evaluation of Highly Potent and Selective Dipeptidyl Peptidase-4 Inhibitors[J]. ARCHIV DER PHARMAZIE,2015,348(6):399-407. |
| APA | Jiang, Tao.,Zhou, Yuren.,Zhu, Jianming.,Chen, Zhuxi.,Sun, Peng.,...&Shen, Jingshan.(2015).Design, Synthesis, and Pharmacological Evaluation of Highly Potent and Selective Dipeptidyl Peptidase-4 Inhibitors.ARCHIV DER PHARMAZIE,348(6),399-407. |
| MLA | Jiang, Tao,et al."Design, Synthesis, and Pharmacological Evaluation of Highly Potent and Selective Dipeptidyl Peptidase-4 Inhibitors".ARCHIV DER PHARMAZIE 348.6(2015):399-407. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。