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.
Copyright © 2010 Elsevier Ltd. All rights reserved.
MeSH terms
-
Animals
-
Diabetes Mellitus, Type 2 / drug therapy
-
Glucagon-Like Peptide 1 / metabolism
-
Hydroxyquinolines / chemical synthesis*
-
Hydroxyquinolines / chemistry
-
Hydroxyquinolines / therapeutic use
-
Mice
-
Quinolines / chemical synthesis
-
Quinolines / chemistry*
-
Quinolines / therapeutic use
-
Receptors, G-Protein-Coupled / agonists*
-
Receptors, G-Protein-Coupled / metabolism
-
Structure-Activity Relationship
-
Thiophenes / chemical synthesis*
-
Thiophenes / chemistry
-
Thiophenes / therapeutic use
Substances
-
Gpbar1 protein, mouse
-
Hydroxyquinolines
-
Quinolines
-
Receptors, G-Protein-Coupled
-
Thiophenes
-
Glucagon-Like Peptide 1
-
quinoline