title: Synthesis and SAR of 2-aryl-3-aminomethylquinolines as agonists of the bile acid receptor TGR5.
abstract: Optimization of a screening hit from uHTS led to the discovery of TGR5 agonist 32, which was shown to have activity in a rodent model for diabetes.
authors.affiliation: Department of Chemistry, Kalypsys, Inc.,10420 Wateridge Circle, San Diego, CA 92121, USA.
authors.forename: Mark R
authors.initials: MR
authors.lastname: Herbert
authors.forename: Dana L
authors.initials: DL
authors.lastname: Siegel
authors.forename: Lena
authors.initials: L
authors.lastname: Staszewski
authors.forename: Charmagne
authors.initials: C
authors.lastname: Cayanan
authors.forename: Urmi
authors.initials: U
authors.lastname: Banerjee
authors.forename: Sangeeta
authors.initials: S
authors.lastname: Dhamija
authors.forename: Jennifer
authors.initials: J
authors.lastname: Anderson
authors.forename: Amy
authors.initials: A
authors.lastname: Fan
authors.forename: Li
authors.initials: L
authors.lastname: Wang
authors.forename: Peter
authors.initials: P
authors.lastname: Rix
authors.forename: Andrew K
authors.initials: AK
authors.lastname: Shiau
authors.forename: Tadimeti S
authors.initials: TS
authors.lastname: Rao
authors.forename: Stewart A
authors.initials: SA
authors.lastname: Noble
authors.forename: Richard A
authors.initials: RA
authors.lastname: Heyman
authors.forename: Eric
authors.initials: E
authors.lastname: Bischoff
authors.forename: Mausumee
authors.initials: M
authors.lastname: Guha
authors.forename: Ayman
authors.initials: A
authors.lastname: Kabakibi
authors.forename: Anthony B
authors.initials: AB
authors.lastname: Pinkerton
mesh_terms: D000818:Animals; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy; D052216:Glucagon-Like Peptide 1 / Q000378:metabolism; D006912:Hydroxyquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D051379:Mice; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D043562:Receptors, G-Protein-Coupled / Q000819:agonists* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use
chemical_list: C513561:Gpbar1 protein, mouse; D006912:Hydroxyquinolines; D011804:Quinolines; D043562:Receptors, G-Protein-Coupled; D013876:Thiophenes; D052216:Glucagon-Like Peptide 1; C037219:quinoline