期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 55, 期 1, 页码 250-267出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm201150j
关键词
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资金
- Ministry of Science and Technology of China [2009ZX09302-001, 2012ZX09304-011]
- Chinese Academy of Sciences [KSCX1-YW-02-2, KSCX2-YW-R-17]
- Natural Science Foundation of China [30628024, 30623008]
- Shanghai Science and Technology Development Fund [074319114, 08DZ2291300, 09DZ2291200]
- CAS-Novo Nordisk
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.
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