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Start Over Author "Zhao, Shizhen" Journal bioorganic & medicinal chemistry
5 results on '"Zhao, Shizhen"'

5. Design, synthesis and evaluation of 1-benzyl-1H-imidazole-5-carboxamide derivatives as potent TGR5 agonists

Author

Wei-Dong Chen, Le Wang, Zhao Shizhen, Ye Wenling, Yan-Dong Wang, Li Xinping, Weiguo Li, and Wenjing Peng

Subjects
Male, medicine.drug_class, Clinical Biochemistry, Pharmaceutical Science, Carboxamide, Pharmacology, 01 natural sciences, Biochemistry, Receptors, G-Protein-Coupled, Mice, Structure-Activity Relationship, chemistry.chemical_compound, In vivo, Drug Discovery, medicine, Animals, Humans, Imidazole, Structure–activity relationship, Secretion, Molecular Biology, Mice, Knockout, Dose-Response Relationship, Drug, Molecular Structure, 010405 organic chemistry, Organic Chemistry, Imidazoles, Glucose Tolerance Test, G protein-coupled bile acid receptor, In vitro, 0104 chemical sciences, Mice, Inbred C57BL, 010404 medicinal & biomolecular chemistry, HEK293 Cells, chemistry, Drug Design, Molecular Medicine, Selectivity
Abstract

TGR5 is emerging as an important and promising target for the treatment of diabetes, obesity and other metabolic syndromes. A series of novel 1-benzyl-1H-imidazole-5-carboxamide derivatives was designed, synthesized and evaluated in vitro and in vivo. The most potent compounds 19d and 19e exhibited excellent agonistic activities against hTGR5, which was superior to those of the reference drugs INT-777 and LCA. In addition, compounds 19d and 19e exhibited good selectivity against FXR and presented significant glucose-lowering effects in vivo. Compound 19d could stimulate GLP-1 secretion by activating of TGR5.

Published
2021

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