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Synthesis, in vitro and in vivo evaluation of 2-aryl-4H-chromene and 3-aryl-1H-benzo[f]chromene derivatives as novel α-glucosidase inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2019 Jan 01; Vol. 29 (1), pp. 119-123. Date of Electronic Publication: 2018 Oct 12. - Publication Year :
- 2019
-
Abstract
- Herein we report a study of novel arylchromene derivatives as analogs of naturally occurring flavonoids with prominent α-glucosidase inhibitory properties. Novel inhibitors were identified via simple stepwise in silico screening, efficient synthesis, and biological evaluation. It is shown that 2-aryl-4H-chromene core retains pharmacophore properties while being readily available synthetically. A lead compound identified through screening inhibits yeast α-glucosidase with IC <subscript>50</subscript> of 62.26 µM and prevents postprandial hyperglycemia in rats at 2.2 mg/kg dose.<br /> (Copyright © 2018 Elsevier Ltd. All rights reserved.)
- Subjects :
- Administration, Oral
Animals
Benzopyrans administration & dosage
Benzopyrans chemistry
Dose-Response Relationship, Drug
Glycoside Hydrolase Inhibitors administration & dosage
Glycoside Hydrolase Inhibitors chemistry
Male
Models, Molecular
Molecular Structure
Rats
Rats, Wistar
Saccharomyces cerevisiae drug effects
Saccharomyces cerevisiae enzymology
Structure-Activity Relationship
Benzopyrans pharmacology
Glycoside Hydrolase Inhibitors pharmacology
alpha-Glucosidases metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 29
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 30340897
- Full Text :
- https://doi.org/10.1016/j.bmcl.2018.10.018