Design, Synthesis, Structure-Activity Relationships, and Docking Studies of 1-(gamma-1,2,3-Triazol Substituted Prolyl)-(S)-3,3-Difluoropyrrolidines as a Novel Series of Potent and Selective Dipeptidyl Peptidase-4 Inhibitors
文献类型：期刊论文
| 作者 | Zhang, Lei1; Su, Mingbo2; Li, Jingya2 ; Ji, Xun1; Wang, Jiang1; Li, Zeng1; Li, Jia2; Liu, Hong1
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| 刊名 | CHEMICAL BIOLOGY & DRUG DESIGN
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| 出版日期 | 2013-02 |
| 卷号 | 81期号:2页码:198-207 |
| 关键词 | dipeptidyl peptidase-4 inhibitor molecular docking triazole type 2 diabetes |
| ISSN号 | 1747-0277 |
| DOI | 10.1111/cbdd.12058 |
| 文献子类 | Article |
| 英文摘要 | Dipeptidyl peptidase-4 inhibitors hold great potential for the treatment of type 2 diabetes. A series of 1-(?-1,2,3-triazol substituted prolyl)-(S)-3,3-difluoropyrrolidines were designed, synthesized, and evaluated as novel dipeptidyl peptidase-4 inhibitors. Most of the compounds exhibited good in vitro potency against dipeptidyl peptidase-4. Among these, compounds 7j, 7q, and 7s displayed good dipeptidyl peptidase-4 activity and excellent selectivity versus other proteases including dipeptidyl peptidase-8, dipeptidyl peptidase-9, and FAP. The possible binding modes of compounds 7j, 7q, and 7s with dipeptidyl peptidase-4 were also explored by molecular docking simulation. |
| WOS关键词 | TYPE-2 DIABETES-MELLITUS ; GLUCAGON-LIKE PEPTIDE-1 ; DPP-4 INHIBITOR ; IV INHIBITOR ; HIGHLY POTENT ; POLYPEPTIDE ; SITAGLIPTIN ; DEGRADATION ; DISCOVERY |
| 资助项目 | National Basic Research Program of China[2009CB940903] ; National Basic Research Program of China[2009CB918502] ; National Natural Science Foundation of China[20721003] ; National Natural Science Foundation of China[81025017] ; National S&T Major Projects[2012ZX09103-101-072] ; Silver Project[260644] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000313529900004 |
| 出版者 | WILEY-BLACKWELL |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277755]  |
| 专题 | 国家新药筛选中心 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 药理学第二研究室 药物化学研究室 药物安全性评价中心 |
| 通讯作者 | Li, Jia |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, State Key Lab Drug Res, Shanghai 200031, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, Natl Ctr Drug Screening, Shanghai 200031, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang, Lei,Su, Mingbo,Li, Jingya,et al. Design, Synthesis, Structure-Activity Relationships, and Docking Studies of 1-(gamma-1,2,3-Triazol Substituted Prolyl)-(S)-3,3-Difluoropyrrolidines as a Novel Series of Potent and Selective Dipeptidyl Peptidase-4 Inhibitors[J]. CHEMICAL BIOLOGY & DRUG DESIGN,2013,81(2):198-207. |
| APA | Zhang, Lei.,Su, Mingbo.,Li, Jingya.,Ji, Xun.,Wang, Jiang.,...&Liu, Hong.(2013).Design, Synthesis, Structure-Activity Relationships, and Docking Studies of 1-(gamma-1,2,3-Triazol Substituted Prolyl)-(S)-3,3-Difluoropyrrolidines as a Novel Series of Potent and Selective Dipeptidyl Peptidase-4 Inhibitors.CHEMICAL BIOLOGY & DRUG DESIGN,81(2),198-207. |
| MLA | Zhang, Lei,et al."Design, Synthesis, Structure-Activity Relationships, and Docking Studies of 1-(gamma-1,2,3-Triazol Substituted Prolyl)-(S)-3,3-Difluoropyrrolidines as a Novel Series of Potent and Selective Dipeptidyl Peptidase-4 Inhibitors".CHEMICAL BIOLOGY & DRUG DESIGN 81.2(2013):198-207. |
入库方式： OAI收割
来源：上海药物研究所
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