Open AccessSynthesis and Inhibitory Effect of Some Indole‐Pyrimidine Based Hybrid Heterocycles on α‐Glucosidase and α‐Amylase as Potential Hypoglycemic Agents
Author(s) -
Badria Farid A.,
Atef Saleh,
AlMajid Abdullah Mohammed,
Ali M.,
Elshaier Yaseen A. M. M.,
Ghabbour Hazem A.,
Islam Mohammad Shahidul,
Barakat Assem
Publication year - 2019
Publication title -
chemistryopen
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.644
H-Index - 29
ISSN - 2191-1363
DOI - 10.1002/open.201900240
Subject(s) - chemistry , barbituric acid , amylase , catalysis , acarbose , indole test , pyrimidine , bimetallic strip , combinatorial chemistry , acetylacetone , yield (engineering) , enzyme , organic chemistry , stereochemistry , materials science , metallurgy
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 IC 50 ( μ M) 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.