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Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 08/2019, Volume 29, Issue 16, pp. 2100 - 2106
We describe here a novel GPR119 agonist , which showed a potent and long-acting hypoglycemic effect in rats via oral dosing. For the discovery of , we chose... 
Spirocyclic | GPR119 agonist | CHEMISTRY, ORGANIC | GLYCEMIC CONTROL | POTENT | CHEMISTRY, MEDICINAL | Cyclohexane | Protein binding | Blood proteins
Journal Article
British Journal of Pharmacology, ISSN 0007-1188, 11/2013, Volume 170, Issue 5, pp. 978 - 990
Background and PurposeG-protein coupled receptor (GPR)55 is a novel lipid sensing receptor activated by both cannabinoid endogenous ligands (endocannabinoids)... 
cells | GPR55 | isolated islets | BRIN | insulin secretion | glucose tolerance | BD11 | lipid agonists | BRIN-BD11 cells | SIGNALING PATHWAYS | CANNABINOID RECEPTOR GPR55 | GPR119 | PROTEIN-COUPLED RECEPTORS | OLEOYLETHANOLAMIDE | ARRIVE GUIDELINES | CB1 RECEPTOR | IN-VIVO | PHARMACOLOGY & PHARMACY | ANTAGONISTS | LANGERHANS | Ethanolamines - pharmacology | Islets of Langerhans - drug effects | Receptors, G-Protein-Coupled - metabolism | Calcium - metabolism | Cannabidiol - analogs & derivatives | Receptors, G-Protein-Coupled - agonists | Dose-Response Relationship, Drug | Receptors, Cannabinoid - drug effects | Receptors, Cannabinoid - metabolism | Resorcinols - pharmacology | Hypoglycemic Agents - toxicity | Insulin-Secreting Cells - metabolism | Piperidines - pharmacology | Time Factors | Islets of Langerhans - metabolism | Clone Cells | Oleic Acids - pharmacology | Palmitic Acids - pharmacology | Cyclic AMP - metabolism | Insulin Secretion | Pyrazoles - pharmacology | Cell Line | Rats | Cannabidiol - pharmacology | Hypoglycemic Agents - pharmacology | Blood Glucose - drug effects | Diabetes Mellitus, Type 2 - blood | Insulin - metabolism | Animals | Diabetes Mellitus, Type 2 - physiopathology | Insulin-Secreting Cells - drug effects | Mice | Blood Glucose - metabolism | Diabetes Mellitus, Type 2 - drug therapy | Immunohistochemistry | Glucose metabolism | Pancreatic beta cells | Analysis | Diabetes | Glucose | Insulin | Dextrose | Research Papers
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 02/2019, Volume 29, Issue 3, pp. 373 - 379
We describe here the generation of a lead compound and its optimization studies that led to the identification of a novel GPR119 agonist. Based on a... 
Spirocyclic structure | GPR119 agonist | GLYCEMIC CONTROL | POTENT | CHEMISTRY, MEDICINAL | SERIES | CHEMISTRY, ORGANIC | DERIVATIVES | DISCOVERY | Cyclohexane | Cytochrome P-450
Journal Article
Bioorganic & Medicinal Chemistry, ISSN 0968-0896, 08/2018, Volume 26, Issue 14, pp. 4080 - 4087
Journal Article
Archiv der Pharmazie, ISSN 0365-6233, 04/2019, Volume 352, Issue 4, pp. e1800267 - n/a
A series of novel orally bioavailable small‐molecule GPR119 agonists with improved potency and moderate physiochemical characteristics were designed,... 
synthesis | type 2 diabetes | biological evaluation | GPR119 | agonistic activity | CHEMISTRY, MEDICINAL | PHARMACOLOGY & PHARMACY | GPR119 AGONISTS | CHEMISTRY, MULTIDISCIPLINARY | Type 2 diabetes | Blood sugar | Analysis | Cyclic adenylic acid | G proteins | Glucose tolerance tests | Membrane proteins
Journal Article
Journal of Computational Chemistry, ISSN 0192-8651, 01/2018, Volume 39, Issue 1, pp. 35 - 41
The GPR119 receptor is a class A G protein‐coupled receptor expressed mainly in pancreatic beta cells. Since GPR119 receptor activation ameliorates Type 2... 
AR231453 | ffTK | CHARMM | GPR119 | parameters | MOLECULAR-DYNAMICS | G-PROTEIN-COUPLED-RECEPTOR-119 | AUTOMATION | GENERAL FORCE-FIELD | CHEMISTRY, MULTIDISCIPLINARY | PROGRAM | Type 2 diabetes | Molecular dynamics | Pancreatic beta cells | Analysis
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 2010, Volume 20, Issue 8, pp. 2577 - 2581
Journal Article