Discovery of a Potent and Orally Efficacious TGR5 Receptor Agonist (original) (raw)
Evaluation of novel TGR5 agonist in combination with Sitagliptin for possible treatment of type 2 diabetes
Suresh Giri
Bioorganic & medicinal chemistry letters, 2018
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Discovery of 3Aryl4-isoxazolecarboxamides as TGR5 Receptor Agonists
David Fraile
Journal of Medicinal Chemistry, 2009
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Novel Small Molecule Agonist of TGR5 Possesses Anti-Diabetic Effects but Causes Gallbladder Filling in Mice
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PloS one, 2015
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TRC210258, a novel TGR5 agonist, reduces glycemic and dyslipidemic cardiovascular risk in animal models of diabesity
Vijay Chauthaiwale
Diabetes, Metabolic Syndrome and Obesity: Targets and Therapy, 2013
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A novel series of indazole-/indole-based glucagon receptor antagonists
Gino Salituro
Bioorganic & Medicinal Chemistry Letters, 2015
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Discovery of a Novel Glucagon Receptor Antagonist N-[(4-{(1S)-1-[3-(3, 5-Dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the Treatment of Type II Diabetes
Mari Candelore
Journal of Medicinal Chemistry, 2012
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Design, Synthesis and Oral Glucose Tolerance Screening of Some 5-substituted benzylidene-3-(2-(2-methyl-1H -benzimidazol- 1-yl)-2-oxoethyl)-1,3-thiazolidine-2,4-dione Derivatives on Rats
Prof Dr Dhrubo Jyoti Sen
American Journal of Advanced Drug Delivery, 2013
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Design, Synthesis, and Antidiabetic Activity of 4-Phenoxynicotinamide and 4-Phenoxypyrimidine-5-carboxamide Derivatives as Potent and Orally Efficacious TGR5 Agonists
mukesh kumawat
Journal of Medicinal Chemistry, 2012
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Discovery of potent, orally active benzimidazole glucagon receptor antagonists
Guoqiang Jiang, Mari Candelore
Bioorganic & Medicinal Chemistry Letters, 2008
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Intestinal TGR5 agonism improves hepatic steatosis and insulin sensitivity in Western diet-fed mice
ERICK ALEXANDER CAMARILLO BLANCO
American Journal of Physiology-Gastrointestinal and Liver Physiology, 2019
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Potent antihyperglycaemic property of a new imidazoline derivative S-22068 (PMS 847) in a rat model of NIDDM
Pierre Renard
British Journal of Pharmacology, 1998
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Discovery of LY3104607: A Potent and Selective G Protein-Coupled Receptor 40 (GPR40) Agonist with Optimized Pharmacokinetic Properties to Support Once Daily Oral Treatment in Patients with Type 2 Diabetes Mellitus
pranab maiti
Journal of medicinal chemistry, 2018
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Discovery of Trifluoromethyl(pyrimidin-2-yl)azetidine-2-carboxamides as Potent, Orally Bioavailable TGR5 (GPBAR1) Agonists: Structure–Activity Relationships, Lead Optimization, and Chronic In Vivo Efficacy
Badry Bursulaya
Journal of Medicinal Chemistry, 2014
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The design and synthesis of a potent glucagon receptor antagonist with favorable physicochemical and pharmacokinetic properties as a candidate for the treatment of type 2 diabetes mellitus
Mary Didiuk
Bioorganic & Medicinal Chemistry Letters, 2013
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Insulinotropic activity of the imidazoline derivative RX871024 in the diabetic GK rat
Robert Bränström
American Journal of …, 2002
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Bariatric surgery reveals a gut-restricted TGR5 agonist that exhibits anti-diabetic effects
Eric Sheu
2020
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Optimization of triazole-based TGR5 agonists towards orally available agents
Kentaro Futatsugi
MedChemComm, 2013
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Synergistic Activity of Thiadiazole And Thiazolidinone Derivatives Against Alloxan Induced Diabetes In Rats
HG Raghavendra
2014
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Mechanism of pure glucose-dependent insulinotropic activity of a novel imidazoline compound BL11282
Vladimir Sharoyko
2008
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Novel Benzylidene Thiazolidinedione Derivatives as Partial PPARγ Agonists and their Antidiabetic Effects on Type 2 Diabetes
Ashok Pattnaik
Scientific Reports, 2017
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Orally efficacious novel small molecule 6-chloro-6-deoxy-1,2,3,4-tetra-O-galloyl- -D-glucopyranose selectively and potently stimulates insulin receptor and alleviates diabetes
Yun Li
Journal of Molecular Endocrinology, 2013
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Novel 5-(Arylideneamino)-1H-Benzo[d]imidazole-2-thiols as Potent Anti-Diabetic Agents: Synthesis, In Vitro α-Glucosidase Inhibition, and Molecular Docking Studies
Sardar Ali
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Natural Compound α-PGG and Its Synthetic Derivative 6Cl-TGQ Alter Insulin Secretion: Evidence for Diminishing Glucose Uptake as a Mechanism
Yanyang Cao
Diabetes, Metabolic Syndrome and Obesity: Targets and Therapy, 2021
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The prelude on novel receptor and ligand targets involved in the treatment of diabetes mellitus
Nilakash Selkar
Advanced pharmaceutical bulletin, 2014
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Identification of Novel Targets of New Insulin Sensitizers- Studies of Related Mechanism With Other Glucose-Lowering Agents
Ihab Nourein, Moawia Elbadri, Mohammed Huneif
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In vivo efficacy of HD0471953: a novel GPR119 agonist for the treatment of type 2 diabetes mellitus
TAE-YOUNG HA
Journal of diabetes research, 2013
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