Design, Synthesis, and Pharmacological Evaluation of Fused beta-Homophenylalanine Derivatives as Potent DPP-4 Inhibitors
文献类型：期刊论文
| 作者 | Jiang, Tao; Zhou, Yuren; Chen, Zhuxi; Sun, Peng; Zhu, Jianming; Zhang, Qiang; Wang, Zhen ; Shao, Qiang; Jiang, Xiangrui; Li, Bo
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| 刊名 | ACS MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2015-05 |
| 卷号 | 6期号:5页码:602-606 |
| 关键词 | Diabetes DPP-4 inhibitor beta-homophenylalanine derivatives sitagliptin |
| ISSN号 | 1948-5875 |
| DOI | 10.1021/acsmedchemlett.5b00074 |
| 文献子类 | Article |
| 英文摘要 | Dipeptidyl peptidase-4 (DPP-4) inhibitors are accepted as a favorable class of agents for the treatment of type 2 diabetes. Herein, a series of fused beta-homophenylalanine derivatives as novel DPP-4 inhibitors were designed, synthesized, and evaluated for their inhibitory activities against DPP-4. Most of them displayed excellent DPP-4 inhibitory activities and good selectivity. Among them, 9aa, 18a, and 18m also showed good efficacy in an oral glucose tolerance test (OGTT) in ICR mice. Moreover, when dosed 8 h prior to glucose challenge, 18m showed significantly greater potency than sitagliptin. It thus provides potential candidates for the further development into potent drugs targeting DPP-4. |
| WOS关键词 | PEPTIDASE-IV INHIBITORS ; DISCOVERY |
| 资助项目 | National Natural Science Foundation of China[21373258] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000354912900024 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276544]  |
| 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,Chen, Zhuxi,et al. Design, Synthesis, and Pharmacological Evaluation of Fused beta-Homophenylalanine Derivatives as Potent DPP-4 Inhibitors[J]. ACS MEDICINAL CHEMISTRY LETTERS,2015,6(5):602-606. |
| APA | Jiang, Tao.,Zhou, Yuren.,Chen, Zhuxi.,Sun, Peng.,Zhu, Jianming.,...&Shen, Jingshan.(2015).Design, Synthesis, and Pharmacological Evaluation of Fused beta-Homophenylalanine Derivatives as Potent DPP-4 Inhibitors.ACS MEDICINAL CHEMISTRY LETTERS,6(5),602-606. |
| MLA | Jiang, Tao,et al."Design, Synthesis, and Pharmacological Evaluation of Fused beta-Homophenylalanine Derivatives as Potent DPP-4 Inhibitors".ACS MEDICINAL CHEMISTRY LETTERS 6.5(2015):602-606. |
入库方式： OAI收割
来源：上海药物研究所
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