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Design, synthesis, structure-activity relationships, and docking studies of pyrazole-containing derivatives as a novel series of potent glucagon receptor antagonists

文献类型：期刊论文

作者Shu, Shuangjie3; Cai, Xiaoqing2; Li, Jia1,3; Feng, Yang2; Dai, Antao2; Wang, Jiang3; Yang, Dehua2,3; Wang, Ming-Wei2,3; Liu, Hong1,3
刊名BIOORGANIC & MEDICINAL CHEMISTRY
出版日期2016-06-15
卷号24期号:12页码:2852-2863
关键词Glucagon receptor Antagonist Molecular docking Pyrazole Type 2 diabetes mellitus
ISSN号0968-0896
DOI10.1016/j.bmc.2016.04.053
文献子类Article
英文摘要Glucagon receptor antagonists possess a great potential for treatment of type 2 diabetes mellitus. A series of pyrazole-containing derivatives were designed, synthesized and evaluated by biological assays as glucagon receptor antagonists. Most of the compounds exhibited good in vitro efficacy. Two of them, compounds 17f and 17k, displayed relatively potent antagonist effects on glucagon receptors with IC50 values of 3.9 and 3.6 mu M, respectively. The possible binding modes of 17f and 17k with the cognate receptor were explored by molecular docking simulation. (C) 2016 Published by Elsevier Ltd.
WOS关键词TYPE-2 ; DISCOVERY ; PANCREAS ; IDENTIFICATION ; METABOLISM ; INTESTINE ; THERAPY ; GENE
资助项目National Natural Science Foundation of China[81220108025] ; National Natural Science Foundation of China[81302633] ; National Natural Science Foundation of China[2147220] ; National Natural Science Foundation of China[91229204] ; SA-SIBS Scholarship Program[00000000] ; National Health and Family Planning Commission[2012ZX09304-011] ; National Health and Family Planning Commission[2013ZX09401003-005] ; National Health and Family Planning Commission[2013ZX09507001] ; National Health and Family Planning Commission[2013ZX09507-002] ; National Health and Family Planning Commission[2014ZX09507002-001] ; Shanghai Science and Technology Development Fund[15DZ2291600] ; Thousand Talents Program in China[00000000]
WOS研究方向Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:000376727800027
出版者PERGAMON-ELSEVIER SCIENCE LTD
源URL[http://119.78.100.183/handle/2S10ELR8/276001]  
专题国家新药筛选中心
药物化学研究室
通讯作者Wang, Ming-Wei; Liu, Hong
作者单位1.China Pharmaceut Univ, Sch Pharm, Nanjing 210009, Jiangsu, Peoples R China
2.Natl Ctr Drug Screening, 189 Guo Shou Jing Rd, Shanghai 201203, Peoples R China;
3.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China;
推荐引用方式
GB/T 7714		 Shu, Shuangjie,Cai, Xiaoqing,Li, Jia,et al. Design, synthesis, structure-activity relationships, and docking studies of pyrazole-containing derivatives as a novel series of potent glucagon receptor antagonists[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2016,24(12):2852-2863.
APA Shu, Shuangjie.,Cai, Xiaoqing.,Li, Jia.,Feng, Yang.,Dai, Antao.,...&Liu, Hong.(2016).Design, synthesis, structure-activity relationships, and docking studies of pyrazole-containing derivatives as a novel series of potent glucagon receptor antagonists.BIOORGANIC & MEDICINAL CHEMISTRY,24(12),2852-2863.
MLA Shu, Shuangjie,et al."Design, synthesis, structure-activity relationships, and docking studies of pyrazole-containing derivatives as a novel series of potent glucagon receptor antagonists".BIOORGANIC & MEDICINAL CHEMISTRY 24.12(2016):2852-2863.

入库方式： OAI收割

来源：上海药物研究所

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