:
Background: The inhibition of α-amylase enzyme is one of the best therapeutic approach for the management of type II
diabetes mellitus. Chalcone possesses a wide range of biological activities.
Objective:
In the current study chalcone derivatives (1-17) were synthesized and evaluated their inhibitory potential against α-amylase
enzyme.
Method:
For that purpose, a library of substituted (E)-1-(naphthalene-2-yl)-3-phenylprop-2-en-1-ones was synthesized by ClaisenSchmidt condensation reaction of 2-acetonaphthanone and substituted aryl benzaldehyde in the presence of base and characterized via
different spectroscopic techniques such as EI-MS, HREI-MS, 1H-, and 13C-NMR.
Results:
Sixteen synthetic chalcones were evaluated for in vitro porcine pancreatic α-amylase inhibition. All the chalcones demonstrated good inhibitory activities in the range of IC50 = 1.25 ± 1.05 to 2.40 ± 0.09 μM as compared to the standard commercial drug
acarbose (IC50 = 1.34 ± 0.3 μM).
Conclusion:
Chalcone derivatives (1-17) were synthesized, characterized, and evaluated for their α-amylase inhibition. SAR revealed
that electron donating groups in the phenyl ring have more influence on enzyme inhibition. However, to insight the participation of
different substituents in the chalcones on the binding interactions with the α-amylase enzyme, in silico (computer simulation) molecular modeling analyses were carried out.
SYNTHESIS OF SOME CHALCONE DERIVATIVES, IN VITRO AND IN SILICO TOXICITY EVALUATION
