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

doi:10.1016/j.bmcl.2018.05.022

CORC > 海洋研究所 > 中国科学院海洋研究所 > 实验海洋生物学重点实验室

	Design, synthesis and biological evaluation of novel pyrimidinedione derivatives as DPP-4 inhibitors
	Li, Ning 1,2,3,4; Wang, Li-Jun 1,2,4; Jiang, Bo 1,2,4; Guo, Shu-Ju 1,2,4; Li, Xiang-Qian 1,2,4; Chen, Xue-Chun 5; Luo, Jiao 1,2,3,4; Li, Chao 1,2,3,4; Wang, Yi5 ; Shi, Da-Yong 1,2,3,4
刊名	BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
	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
DOI	10.1016/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
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000434468000003
内容类型	期刊论文
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.