Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10590993 | Bioorganic & Medicinal Chemistry Letters | 2014 | 5 Pages |
Abstract
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 improved potency, compared to a reference compound with a pyridine scaffold. The pharmacokinetic profile of the representative compound 18 was considered moderate.
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Authors
Eun Ju Park, Young Gil Ahn, Seung Hyun Jung, Hyo Jeong Bang, Mira Kim, Dong Jin Hong, Jisook Kim, Kwee Hyun Suh, Young Jin Kim, Doran Kim, Eun-Yeong Kim, Kiho Lee, Kyung Hoon Min,