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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
2018-07-01
Source PublicationBIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN0960-894X
Volume28Issue:12Pages:2131-2135
Corresponding AuthorWang, Yi(mysky@zju.edu.cn) ; Shi, Da-Yong(shidayong@qdio.ac.cn)
AbstractA 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.
KeywordPyrimidinedionederivatives DPP-4 inhibitor Molecular hybrid SARs Type 2 diabetes
DOI10.1016/j.bmcl.2018.05.022
Indexed BySCI
Language英语
Funding ProjectNational 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 AreaPharmacology & Pharmacy ; Chemistry
WOS SubjectChemistry, Medicinal ; Chemistry, Organic
WOS IDWOS:000434468000003
PublisherPERGAMON-ELSEVIER SCIENCE LTD
Citation statistics
Cited Times:1[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.qdio.ac.cn/handle/337002/159187
Collection实验海洋生物学重点实验室
Corresponding AuthorWang, Yi; Shi, Da-Yong
Affiliation1.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 AffilicationKey Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese Academy of Sciences
Corresponding Author AffilicationKey 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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