Optimisation of novel 4, 8-disubstituted dihydropyrimido[5,4-b][1,4]oxazine derivatives as potent GPR 119 agonists

Clicks: 161
ID: 275478
2020
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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-][1,4]oxazine derivatives as GPR119 agonists. Most designed compounds exhibited good agonistic activities. Among them, compound and demonstrated the potent EC values (13 and 12 nM, respectively) and strong inherent activities. Moreover, significant hypoglycaemic effect of compound was observed by reducing the blood glucose AUC at the dose of 30 mg/kg, which is stronger than Vildagliptin (23.4% reduction vs. 17.9% reduction).
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fang2020optimisationjournal Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Fang, Y.
Journal Journal of enzyme inhibition and medicinal chemistry
Year 2020
DOI
10.1080/14756366.2019.1681988
URL
Keywords Keywords not found

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