Evaluation of anti-diabetic effect and gall bladder function with 2-thio-5-thiomethyl substituted imidazoles as TGR5 receptor agonists

A novel series of 2-thio-5-thiomethyl substituted imidazoles was discovered to be potent TGR5 agonists that possessed glucose-lowering effects while inhibiting gall bladder emptying in mice. [Display omitted] A novel series of 2-thio-5-thiomethyl substituted imidazoles was discovered to be potent TG...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2017-04, Vol.27 (8), p.1760-1764
Hauptverfasser:	Zhang, Xuqing, Sui, Zhihua, Kauffman, Jack, Hou, Cuifen, Chen, Cailin, Du, Fuyong, Kirchner, Thomas, Liang, Yin, Johnson, Dana, Murray, William V., Demarest, Keith
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Blood Glucose - analysis Blood Glucose - metabolism Cell Line Diabetes Mellitus - blood Diabetes Mellitus - drug therapy Diabetes Mellitus - metabolism Diabetes Mellitus - physiopathology Gall bladder Gallbladder Emptying - drug effects Humans Hypoglycemic Agents - chemistry Hypoglycemic Agents - pharmacology Hypoglycemic Agents - therapeutic use Imidazole Imidazoles - chemistry Imidazoles - pharmacology Imidazoles - therapeutic use Methylation Mice Mice, Inbred C57BL OGTT Receptors, G-Protein-Coupled - agonists Receptors, G-Protein-Coupled - metabolism TGR5
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Zusammenfassung:	A novel series of 2-thio-5-thiomethyl substituted imidazoles was discovered to be potent TGR5 agonists that possessed glucose-lowering effects while inhibiting gall bladder emptying in mice. [Display omitted] A novel series of 2-thio-5-thiomethyl substituted imidazoles was discovered to be potent TGR5 agonists that possessed glucose-lowering effects while inhibiting gall bladder emptying in mice.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2017.02.069