title: Evaluation of anti-diabetic effect and gall bladder function with 2-thio-5-thiomethyl substituted imidazoles as TGR5 receptor agonists.
abstract: 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.
authors.affiliation: Cardiovascular and Metabolic Research, Janssen Research & Development, LLC, Welsh & McKean Roads, Box 776, Spring House, PA 19477, United States. Electronic address: xzhang5@its.jnj.com.
authors.forename: Xuqing
authors.initials: X
authors.lastname: Zhang
authors.affiliation: Cardiovascular and Metabolic Research, Janssen Research & Development, LLC, Welsh & McKean Roads, Box 776, Spring House, PA 19477, United States.
authors.forename: Zhihua
authors.initials: Z
authors.lastname: Sui
authors.affiliation: Cardiovascular and Metabolic Research, Janssen Research & Development, LLC, Welsh & McKean Roads, Box 776, Spring House, PA 19477, United States.
authors.forename: Jack
authors.initials: J
authors.lastname: Kauffman
authors.affiliation: Cardiovascular and Metabolic Research, Janssen Research & Development, LLC, Welsh & McKean Roads, Box 776, Spring House, PA 19477, United States.
authors.forename: Cuifen
authors.initials: C
authors.lastname: Hou
authors.affiliation: Cardiovascular and Metabolic Research, Janssen Research & Development, LLC, Welsh & McKean Roads, Box 776, Spring House, PA 19477, United States.
authors.forename: Cailin
authors.initials: C
authors.lastname: Chen
authors.affiliation: Cardiovascular and Metabolic Research, Janssen Research & Development, LLC, Welsh & McKean Roads, Box 776, Spring House, PA 19477, United States.
authors.forename: Fuyong
authors.initials: F
authors.lastname: Du
authors.affiliation: Cardiovascular and Metabolic Research, Janssen Research & Development, LLC, Welsh & McKean Roads, Box 776, Spring House, PA 19477, United States.
authors.forename: Thomas
authors.initials: T
authors.lastname: Kirchner
authors.affiliation: Cardiovascular and Metabolic Research, Janssen Research & Development, LLC, Welsh & McKean Roads, Box 776, Spring House, PA 19477, United States.
authors.forename: Yin
authors.initials: Y
authors.lastname: Liang
authors.affiliation: Cardiovascular and Metabolic Research, Janssen Research & Development, LLC, Welsh & McKean Roads, Box 776, Spring House, PA 19477, United States.
authors.forename: Dana
authors.initials: D
authors.lastname: Johnson
authors.affiliation: Cardiovascular and Metabolic Research, Janssen Research & Development, LLC, Welsh & McKean Roads, Box 776, Spring House, PA 19477, United States.
authors.forename: William V
authors.initials: WV
authors.lastname: Murray
authors.affiliation: Cardiovascular and Metabolic Research, Janssen Research & Development, LLC, Welsh & McKean Roads, Box 776, Spring House, PA 19477, United States.
authors.forename: Keith
authors.initials: K
authors.lastname: Demarest
mesh_terms: D000818:Animals; D001786:Blood Glucose / Q000032:analysis / Q000378:metabolism; D002460:Cell Line; D003920:Diabetes Mellitus / Q000097:blood / Q000188:drug therapy* / Q000378:metabolism / Q000503:physiopathology; D016473:Gallbladder Emptying / Q000187:drug effects*; D006801:Humans; D007004:Hypoglycemic Agents / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D007093:Imidazoles / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D008745:Methylation; D051379:Mice; D008810:Mice, Inbred C57BL; D043562:Receptors, G-Protein-Coupled / Q000819:agonists* / Q000378:metabolism
chemical_list: D001786:Blood Glucose; C473772:GPBAR1 protein, human; D007004:Hypoglycemic Agents; D007093:Imidazoles; D043562:Receptors, G-Protein-Coupled
keywords: Gall bladder; Imidazole; OGTT; TGR5