Design, Synthesis, and Structure–Activity Relationships of 3, 4, 5??Trisubstituted 4, 5??Dihydro??1, 2, 4??oxadiazoles as TGR5 Agonists

…, Y Feng, Q Zou, T Kurtán, Y Leng, J Shen

Index: Zhu, Junjie; Ye, Yangliang; Ning, Mengmeng; Mandi, Attila; Feng, Ying; Zou, Qingan; Kurtan, Tibor; Leng, Ying; Shen, Jianhua ChemMedChem, 2013 , vol. 8, # 7 p. 1210 - 1223

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Citation Number: 13

Abstract

Given its role in the mediation of energy and glucose homeostasis, the G-protein-coupled bile acid receptor 1 (TGR5) is considered a potential target for the treatment of type 2 diabetes mellitus and other metabolic disorders. By thorough analysis of diverse structures of published TGR5 agonists, a hypothetical ligand-based pharmacophore model was built, and a new class of potent TGR5 agonists, based on the novel 3,4,5-trisubstituted 4,5-dihydro-1,2,4-oxadiazole core, ...

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