Abstract
The Michael addition reaction of barbituric acid with chalcones incorporating the indole scaffold was achieved by using a highly efficient bimetallic Iron–palladium catalyst in the presence of acetylacetone (acac). This catalytic approach produced the desired products in a simple operation and low catalyst loading with acceptable yield of the new hybrids. All tested compounds were subjected for biological activity on α‐glucosidase and α‐amylase. The results revealed that all synthesized compounds exhibited very good activity against both enzymes when compared to positive control (acarbose). Moreover, compound 5o showed the best activity whereas its IC50 (μM) are 13.02+0.01 and 21.71+0.82 for α‐glucosidase and α‐amylase respectively. Both compounds 5o and 5l exhibited high similarity in binding mode and pose with amylase protein (4UAC). The obtained data may be used for developing potential hypoglycemic agents.
Highlights
The Michael addition reaction of barbituric acid with chalcones synthesized compounds exhibited very good activity against incorporating the indole scaffold was achieved by using a both enzymes when compared to positive control. highly efficient bimetallic Iron–palladium catalyst in the pres- compound 5o showed the best activity whereas its ence of acetylacetone
The results revealed that all developing potential hypoglycemic agents
Rapidly, whereas α-glucosidase breaks these shorter chains into free glucose
Summary
Synthesis the desired product in moderate yield (55 %) (Table 1). To investigate the generality of this method, the reaction of of N-alkyl-3-acetylindole and aryl aldehyde derivatives stirring barbituric acid and different enones was examined under the in EtOH/H2O (1 : 1) with NaOH at room temperature for 24 h. Optimized reaction conditions (10 mol% of FeCl3, 10 mol% of 37 The product was produced in high yield (up to 90 %), as PdCl2 and 15 mol% Acac, 1.0 equiv. The configuration of the chalcones barbituric acid in CH3OH at at 60 °C. These compounds was supposed in analogy with similar compounds, previously prepared by us, whose configuration
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
