期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 28, 期 12, 页码 2131-2135出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2018.05.022
关键词
Pyrimidinedionederivatives; DPP-4 inhibitor; Molecular hybrid; SARs; Type 2 diabetes
资金
- National Natural Science Foundation of China [81773586, 81703354]
- Shandong Provincial Natural Science Foundation for Distinguished Young Scholars [JQ201722]
- Key research and development project of Shandong province [2016GSF201193, 2016ZDJS07A13, 2016GSF115002, 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, 2017-CXZX01-3-9]
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.
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