| Literature DB >> 22103243 |
Qing Liu1, Na Li, Yunyun Yuan, Huili Lu, Xiaoyan Wu, Caihong Zhou, Min He, Haoran Su, Meng Zhang, Jia Wang, Bao Wang, You Wang, Dawei Ma, Yang Ye, Hans-Christoph Weiss, Ernst R F Gesing, Jiayu Liao, Ming-Wei Wang.
Abstract
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.Entities:
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Year: 2011 PMID： 22103243 DOI： 10.1021/jm201150j
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446