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Design, synthesis and biological evaluation of novel pyrimidinedione derivatives as DPP-4 inhibitors

文献类型：期刊论文

作者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
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
出版日期2018-07-01
卷号28期号:12页码:2131-2135
关键词Pyrimidinedionederivatives DPP-4 inhibitor Molecular hybrid SARs Type 2 diabetes
ISSN号0960-894X
DOI10.1016/j.bmcl.2018.05.022
通讯作者Wang, Yi(mysky@zju.edu.cn) ; Shi, Da-Yong(shidayong@qdio.ac.cn)
英文摘要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.
资助项目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研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:000434468000003
出版者PERGAMON-ELSEVIER SCIENCE LTD
源URL[http://ir.qdio.ac.cn/handle/337002/159186]  
专题海洋研究所_实验海洋生物学重点实验室
通讯作者Wang, Yi; Shi, Da-Yong
作者单位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
推荐引用方式
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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来源：海洋研究所

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