| 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
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| Source Publication | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| ISSN | 0960-894X
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| 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
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| Indexed By | SCI
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| Language | 英语
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| 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]
; 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
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| WOS Subject | Chemistry, Medicinal
; Chemistry, Organic
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| WOS ID | WOS:000434468000003
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| Publisher | PERGAMON-ELSEVIER SCIENCE LTD
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| Citation statistics |
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| Document Type | 期刊论文
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| Identifier | http://ir.qdio.ac.cn/handle/337002/159187
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| 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
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| First Author Affilication | Key Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese Academy of Sciences
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| Corresponding Author Affilication | Key Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese Academy of Sciences
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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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