1352203-90-7Relevant articles and documents
Cyclobutane derivatives as novel nonpeptidic small molecule agonists of glucagon-like peptide-1 receptor
Liu, Qing,Li, Na,Yuan, Yunyun,Lu, Huili,Wu, Xiaoyan,Zhou, Caihong,He, Min,Su, Haoran,Zhang, Meng,Wang, Jia,Wang, Bao,Wang, You,Ma, Dawei,Ye, Yang,Weiss, Hans-Christoph,Gesing, Ernst R. F.,Liao, Jiayu,Wang, Ming-Wei
, p. 250 - 267 (2012/03/10)
A novel cyclobutane class of nonpeptidic glucagon-like peptide-1 (GLP-1) receptor agonists, exemplified by 3, was identified using receptor binding and multiple response element/cAMP response element (MRE/CRE)-driven reporter gene assays. The structures of 3 and its three isomers were elucidated by NMR, HRESIMS, and X-ray crystallography. A series of structural modifications were also made based on the core structure of 3 with different substitution groups at the west and east ends. Among these analogues, compound 16 was found to be 4- to 5-fold more potent than 3 both in vitro and in vivo.