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

Author

Fang, Yuanying, Zhang, Shaokun, Li, Min, Xiong, Lijuan, Tu, Liangxing, Xie, Saisai, Jin, Yi, Liu, Yanhua, Yang, Zunhua, and Liu, Ronghua

Subjects
OXAZINES, BLOOD sugar, TYPE 2 diabetes, DIABETES
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 EC50 values (13 and 12 nM, respectively) and strong inherent activities. Moreover, significant hypoglycaemic effect of compound 15 was observed by reducing the blood glucose AUC0–2h at the dose of 30 mg/kg, which is stronger than Vildagliptin (23.4% reduction vs. 17.9% reduction). [ABSTRACT FROM AUTHOR]

Published
2020
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8. Optimisation of novel 4, 8-disubstituted dihydropyrimido[5,4- b ][1,4]oxazine derivatives as potent GPR 119 agonists.

Author

Fang Y, Zhang S, Li M, Xiong L, Tu L, Xie S, Jin Y, Liu Y, Yang Z, and Liu R

Subjects
Animals, Blood Glucose drug effects, Dose-Response Relationship, Drug, Glucose Tolerance Test, Humans, Hypoglycemic Agents chemical synthesis, Hypoglycemic Agents chemistry, Mice, Mice, Inbred C57BL, Molecular Structure, Oxazines chemical synthesis, Oxazines chemistry, Pyrimidines chemical synthesis, Pyrimidines chemistry, Structure-Activity Relationship, Hypoglycemic Agents pharmacology, Oxazines pharmacology, Pyrimidines pharmacology, Receptors, G-Protein-Coupled agonists
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 50 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 0-2h at the dose of 30 mg/kg, which is stronger than Vildagliptin (23.4% reduction vs. 17.9% reduction).

Published
2020
Full Text
View/download PDF

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