Synthesis and SAR studies of bicyclic amine series GPR119 agonists

We disclosed a novel series of G-protein coupled receptor 119 (GPR119) agonists based on a bicyclic amine scaffold. Through the optimization of hit compound 1, we discovered that the basic nitrogen atom of bicyclic amine played an important role in GPR119 agonist activity expression and that an inda...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2012-08, Vol.22 (15), p.5123-5128
Hauptverfasser:	Sakairi, Masao, Kogami, Masakazu, Torii, Masafumi, Kataoka, Hiroyo, Fujieda, Hiroki, Makino, Mitsuhiro, Kataoka, Daisuke, Okamoto, Ryuji, Miyazawa, Toshiyuki, Okabe, Morio, Inoue, Megumi, Takahashi, Naoki, Harada, Satoko, Watanabe, Nobuhide
Format:	Artikel
Sprache:	eng
Schlagworte:	agonists Amines - chemical synthesis Amines - chemistry Amines - pharmacology animal models Animals Basic nitrogen Bicyclic amine Biological and medical sciences blood glucose Blood Glucose - drug effects Blood Glucose - metabolism Bridged Bicyclo Compounds - chemistry chemistry G-protein coupled receptors Glucose Tolerance Test glycemic control GPR119 GPR119 agonist Humans Hypoglycemic Agents - chemical synthesis Hypoglycemic Agents - chemistry Hypoglycemic Agents - pharmacology Indanone Indans - chemical synthesis Indans - chemistry Indans - pharmacology Medical sciences Mice Mice, Inbred C57BL nitrogen oGTT Pharmacology. Drug treatments Protein Binding Pyrimidines - chemical synthesis Pyrimidines - chemistry Pyrimidines - pharmacology Receptors, G-Protein-Coupled - agonists Receptors, G-Protein-Coupled - metabolism scGTT Structure-Activity Relationship
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