Synthesis and biological evaluation of novel benzyl-substituted (S)-phenylalanine derivatives as potent dipeptidyl peptidase 4 inhibitors
文献类型：期刊论文
| 作者 | Liu, Yang2; Si, Meimei1; Tang, Li2; Shangguan, Shihao2; Wu, Haoshu1; Li, Jia3 ; Wu, Peng2; Ma, Xiaodong2; Liu, Tao2; Hu, Yongzhou2
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2013-09-15 |
| 卷号 | 21期号:18页码:5679-5687 |
| 关键词 | Dipeptidyl peptidase 4 inhibitors Type 2 diabetes 1,2,3-Triazole (S)-Phenylalanine derivatives Selectivity |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2013.07.034 |
| 文献子类 | Article |
| 英文摘要 | A series of novel benzyl-substituted (S)-phenylalanine derivatives were synthesized and evaluated for their dipeptidyl peptidase 4 (DPP-4) inhibitory activity and selectivity. It was found that most synthesized target compounds were potent DPP-4 inhibitors with IC50 values in 3.79-25.52 nM, which were significantly superior to that of the marketed drug sitagliptin. Furthermore, the 4-fluorobenzyl substituted phenylalanine derivative 6g not only displayed the potent DPP-4 inhibition with an IC50 value of 3.79 nM, but also showed better selectivity against DPP-4 over other related enzymes including DPP-7, DPP-8, and DPP-9. In an oral glucose tolerance test (OGTT) in normal Sprague Dawley rats, compound 6g reduced blood glucose excursion in a dose-dependent manner. (C) 2013 Elsevier Ltd. All rights reserved. |
| WOS关键词 | DPP-IV INHIBITORS ; MEDICINAL CHEMISTRY ; HIGHLY POTENT ; DISCOVERY |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000323803900004 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277461]  |
| 专题 | 药物化学研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药物安全性评价中心 国家新药筛选中心 |
| 通讯作者 | Liu, Tao |
| 作者单位 | 1.Zhejiang Univ, Coll Pharmaceut Sci, Inst Pharmacol & Toxicol, Hangzhou 310058, Zhejiang, Peoples R China; 2.Zhejiang Univ, Coll Pharmaceut Sci, ZJU ENS Joint Lab Med Chem, Hangzhou 310058, Zhejiang, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Chinese Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Liu, Yang,Si, Meimei,Tang, Li,et al. Synthesis and biological evaluation of novel benzyl-substituted (S)-phenylalanine derivatives as potent dipeptidyl peptidase 4 inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2013,21(18):5679-5687. |
| APA | Liu, Yang.,Si, Meimei.,Tang, Li.,Shangguan, Shihao.,Wu, Haoshu.,...&Hu, Yongzhou.(2013).Synthesis and biological evaluation of novel benzyl-substituted (S)-phenylalanine derivatives as potent dipeptidyl peptidase 4 inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY,21(18),5679-5687. |
| MLA | Liu, Yang,et al."Synthesis and biological evaluation of novel benzyl-substituted (S)-phenylalanine derivatives as potent dipeptidyl peptidase 4 inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY 21.18(2013):5679-5687. |
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。