Institutional Repository of Key Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese Academy of Sciences
| Design, synthesis and biological evaluation of novel pyrimidinedione derivatives as DPP-4 inhibitors | |
Li, Ning1,2,3,4; Wang, Li-Jun1,2,4; Jiang, Bo1,2,4; Guo, Shu-Ju1,2,4; Li, Xiang-Qian1,2,4; Chen, Xue-Chun5; Luo, Jiao1,2,3,4; Li, Chao1,2,3,4; Wang, Yi5 ; Shi, Da-Yong1,2,3,4
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| 2018-07-01 | |
| Source Publication | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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| ISSN | 0960-894X |
| Volume | 28Issue:12Pages:2131-2135 |
| Corresponding Author | Wang, Yi(mysky@zju.edu.cn) ; Shi, Da-Yong(shidayong@qdio.ac.cn) |
| Abstract | A series of novel pyrimidinedione derivatives were designed and evaluated for in vitro dipeptidyl peptidase-4 (DPP-4) inhibitory activity and in vivo anti-hyperglycemic efficacy. Among them, the representative compounds 11, 15 and 16 showed excellent inhibitory activity of DPP-4 with IC50 values of 64.47 nM, 188.7 nM and 65.36 nM, respectively. Further studies revealed that compound 11 was potent in vivo hypoglycemic effect. The structure-activity relationships of these pyrimidinedione derivatives had been discussed, which would be useful for developing novel DPP-4 inhibitors as treating type 2 diabetes. |
| Keyword | Pyrimidinedionederivatives DPP-4 inhibitor Molecular hybrid SARs Type 2 diabetes |
| DOI | 10.1016/j.bmcl.2018.05.022 |
| Indexed By | SCI |
| Language | 英语 |
| Funding Project | National Natural Science Foundation of China[81773586] ; National Natural Science Foundation of China[81703354] ; Shandong Provincial Natural Science Foundation for Distinguished Young Scholars[JQ201722] ; Key research and development project of Shandong province[2016GSF201193] ; Key research and development project of Shandong province[2016ZDJS07A13] ; Key research and development project of Shandong province[2016GSF115002] ; Key research and development project of Shandong province[2016GSF115009] ; Key Research Program of Frontier Sciences, CAS[QYZDB-SSW-DQC014] ; Project of Discovery, Evaluation and Transformation of Active Natural Compounds, Strategic Biological Resources Service Network Program of Chinese Academy of Sciences[ZSTH-026] ; National Science Foundation of China (NSFC)-Shandong Joint Fund[U1706213] ; National Program for Support of Top-notch Young Professionals ; Taishan scholar Youth Project of Shandong province and Qingdao Marine Biomedical Science and Technology Innovation Center project[2017-CXZX01-1-1] ; Taishan scholar Youth Project of Shandong province and Qingdao Marine Biomedical Science and Technology Innovation Center project[2017-CXZX01-3-9] |
| WOS Research Area | Pharmacology & Pharmacy ; Chemistry |
| WOS Subject | Chemistry, Medicinal ; Chemistry, Organic |
| WOS ID | WOS:000434468000003 |
| Publisher | PERGAMON-ELSEVIER SCIENCE LTD |
| Citation statistics | |
| Document Type | 期刊论文 |
| Identifier | http://ir.qdio.ac.cn/handle/337002/159187 |
| Collection | 实验海洋生物学重点实验室 |
| Corresponding Author | Wang, Yi; Shi, Da-Yong |
| Affiliation | 1.Chinese Acad Sci, Inst Oceanol, Key Lab Expt Marine Biol, Qingdao 266071, Peoples R China 2.Qingdao Natl Lab Marine Sci & Technol, Lab Marine Drugs & Bioprod, Qingdao 266235, Peoples R China 3.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 4.Chinese Acad Sci, Ctr Ocean Mega Sci, Qingdao 266071, Peoples R China 5.Zhejiang Univ, Coll Pharmaceut Sci, Hangzhou 310058, Zhejiang, Peoples R China |
| First Author Affilication | Key Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese Academy of Sciences |
| Corresponding Author Affilication | Key Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese Academy of Sciences |
| Recommended Citation GB/T 7714 | Li, Ning,Wang, Li-Jun,Jiang, Bo,et al. Design, synthesis and biological evaluation of novel pyrimidinedione derivatives as DPP-4 inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2018,28(12):2131-2135. |
| APA | Li, Ning.,Wang, Li-Jun.,Jiang, Bo.,Guo, Shu-Ju.,Li, Xiang-Qian.,...&Shi, Da-Yong.(2018).Design, synthesis and biological evaluation of novel pyrimidinedione derivatives as DPP-4 inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,28(12),2131-2135. |
| MLA | Li, Ning,et al."Design, synthesis and biological evaluation of novel pyrimidinedione derivatives as DPP-4 inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 28.12(2018):2131-2135. |
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| File Name/Size | DocType | Version | Access | License | ||
| Design, synthesis an（824KB） | 期刊论文 | 出版稿 | 开放获取 | CC BY-NC-SA | View Application Full Text | |
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