Synthesis and biological evaluation of azobicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes
Cho, Tang Peng2; Long, Yang Fang2; Gang, Lin Zhi2; Yang, Wang2; Jun, Lu He2; Yuan, Shen Guang2; Hong, Fu Jian2; Lin, Wang2; Liang, Guan Dong2; Lei, Zhang2
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
2010-06-15
卷号20期号:12页码:3565-3568
关键词Azobicyclo[3.3.0]octane derivatives Dipeptidyl peptidase 4 Oral glucose tolerance test Type 2 diabetes mellitus
ISSN号0960-894X
DOI10.1016/j.bmcl.2010.04.120
文献子类Article
英文摘要A series of novel azobicyclo[3.3.0]octane derivatives were synthesized and evaluated as dipeptidyl peptidase 4 (DPP-4) inhibitors. The effort resulted in the discovery of inhibitor 2a, which exhibited excellent efficacies in an oral glucose tolerance test. Introduction of methyl group (2j) could prolong the inhibition of serum DPP-4 activity. (C) 2010 Elsevier Ltd. All rights reserved.
WOS关键词DPP-IV INHIBITORS ; ANTIHYPERGLYCEMIC PROPERTIES ; POTENT ; GLP-1 ; SAXAGLIPTIN ; CONVERSION
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
出版者PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号WOS:000278208200024
内容类型期刊论文
源URL[http://119.78.100.183/handle/2S10ELR8/278871]  
专题药理学第一研究室
中科院受体结构与功能重点实验室
新药研究国家重点实验室
通讯作者Cho, Tang Peng
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
2.Shanghai Hengrui Pharmaceut Co Ltd, Shanghai 200245, Peoples R China;
推荐引用方式
GB/T 7714
Cho, Tang Peng,Long, Yang Fang,Gang, Lin Zhi,et al. Synthesis and biological evaluation of azobicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2010,20(12):3565-3568.
APA Cho, Tang Peng.,Long, Yang Fang.,Gang, Lin Zhi.,Yang, Wang.,Jun, Lu He.,...&Tai, Mong Xian.(2010).Synthesis and biological evaluation of azobicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,20(12),3565-3568.
MLA Cho, Tang Peng,et al."Synthesis and biological evaluation of azobicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 20.12(2010):3565-3568.
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