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New 6-amino-pyrido[2,3-d]pyrimidine-2,4-diones as novel agents to treat type 2 diabetes: A simple and efficient synthesis, α-glucosidase inhibition, molecular modeling and kinetic study.
- Source :
-
European Journal of Medicinal Chemistry . Jul2018, Vol. 155, p353-363. 11p. - Publication Year :
- 2018
-
Abstract
- A new series of 6-amino-pyrido[2,3-d]pyrimidine-2,4-dione derivatives 3a – 3s were prepared via a facile and efficient reaction from α -azidochalcones and 6-amiouracils. The reactions were performed under mild conditions to produce the corresponding compounds in good to excellent yields. Obtained derivatives 3a – 3s were evaluated for α-glucosidase inhibitory activity and all of them exhibited excellent in vitro yeast α -glucosidase inhibition with IC 50 values ranging from 78.0 ± 2.0 to 252.4 ± 1.0 μM. For example, the most active compound 3o was around 10-fold more potent than acarbose, a standard drug (IC 50 = 750.0 ± 1.5 μM). Kinetic study of compound 3o revealed that it inhibited α -glucosidase in a competitive mode. Molecular modeling studies of the most active compounds 3o , 3i , 3e and 3m were also performed. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 02235234
- Volume :
- 155
- Database :
- Academic Search Index
- Journal :
- European Journal of Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 130858411
- Full Text :
- https://doi.org/10.1016/j.ejmech.2018.05.046