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Optimisation of novel 4, 8-disubstituted dihydropyrimido[5,4-b][1,4]oxazine derivatives as potent GPR 119 agonists.
- Source :
- Journal of Enzyme Inhibition & Medicinal Chemistry; Dec2020, Vol. 35 Issue 1, p50-58, 9p
- Publication Year :
- 2020
-
Abstract
- GPR119 is a promising target for discovery of anti-type 2 diabetes mellitus agents. We described the optimisation of a novel series of pyrimido[5,4-b][1,4]oxazine derivatives as GPR119 agonists. Most designed compounds exhibited good agonistic activities. Among them, compound 10 and 15 demonstrated the potent EC<subscript>50</subscript> values (13 and 12 nM, respectively) and strong inherent activities. Moreover, significant hypoglycaemic effect of compound 15 was observed by reducing the blood glucose AUC<subscript>0–2h</subscript> at the dose of 30 mg/kg, which is stronger than Vildagliptin (23.4% reduction vs. 17.9% reduction). [ABSTRACT FROM AUTHOR]
- Subjects :
- OXAZINES
BLOOD sugar
TYPE 2 diabetes
DIABETES
Subjects
Details
- Language :
- English
- ISSN :
- 14756366
- Volume :
- 35
- Issue :
- 1
- Database :
- Complementary Index
- Journal :
- Journal of Enzyme Inhibition & Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 147176692
- Full Text :
- https://doi.org/10.1080/14756366.2019.1681988