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Discovery of novel pyrimidine and malonamide derivatives as TGR5 agonists
- Authors
- 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
- Issue Date
- Sep-2014
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- TGR5; Pyrimidine; Malonamide; Agonist; Bioisostere
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.24, no.17, pp 4271 - 4275
- Pages
- 5
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 24
- Number
- 17
- Start Page
- 4271
- End Page
- 4275
- ISSN
- 0960-894X
1464-3405
- 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. (C) 2014 Elsevier Ltd. All rights reserved.
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