Discovery of novel pyrimidine and malonamide derivatives as TGR5 agonists

Takeda G-protein-coupled receptor 5 (TGR5) is a promising molecular target for metabolic diseases. A series of 4-(2,5-dichlorophenoxy)pyrimidine and cyclopropylmalonamide derivatives were synthesized as potent agonists of TGR5 based on a bioisosteric replacement strategy. Several compounds exhibited...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2014-09, Vol.24 (17), p.4271-4275
Hauptverfasser:	Park, Eun Ju, Ahn, Young Gil, Jung, Seung Hyun, Bang, Hyo Jeong, Kim, Mira, Hong, Dong Jin, Kim, Jisook, Suh, Kwee Hyun, Kim, Young Jin, Kim, Doran, Kim, Eun-Yeong, Lee, Kiho, Min, Kyung Hoon
Format:	Artikel
Sprache:	eng
Schlagworte:	Agonist Animals Bioisostere Biological Availability Cytochrome P-450 Enzyme Inhibitors - administration & dosage Cytochrome P-450 Enzyme Inhibitors - chemistry Cytochrome P-450 Enzyme Inhibitors - pharmacology Cytochrome P-450 Enzyme System - metabolism Dose-Response Relationship, Drug Drug Discovery HEK293 Cells Humans Malonamide Malonates - administration & dosage Malonates - chemistry Malonates - pharmacology Mice Mice, Inbred ICR Microsomes, Liver - drug effects Microsomes, Liver - enzymology Microsomes, Liver - metabolism Molecular Structure Pyrimidine Pyrimidines - administration & dosage Pyrimidines - chemistry Pyrimidines - pharmacology Receptors, G-Protein-Coupled - agonists Structure-Activity Relationship TGR5
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