عنوان
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Synthesis, Structural Studies, and Glucosidase Inhibitory, Antidiabetic, and Antioxidant Activities of 2,3-Dihydroquinazolin4(1H)ones Derived from Pyrazol-4-carbaldehyde and Anilines
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چکیده
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A series of new quinazoline derivatives were designed
and synthesized via a one-pot condensation reaction between isatoic
anhydride and aromatic aldehydes with anilines using aluminum
sulfate as a catalyst in refluxing ethanol. Their structures were
confirmed by their physical, IR, 1H NMR, 13C NMR, and mass
spectroscopy data and evaluated for some biological effects,
including the antioxidant and ?-glucosidase inhibitory activities as
well as some in vivo hematological parameters. The ability of
synthesized compounds in the inhibition of ?-glucosidase was also
investigated through the in silico study. The significant and
important changes in some hematological tests were perceived.
Notably, compound 4h showed more reducing effects on
cholesterol and triglyceride levels. This molecule certainly has the
potential to be developed as the antihyperlipemic compound. The
tested compounds, in particular, compounds 4j and 4l, were found to be uniquely reducing blood sugar levels. The entire
synthesized compounds showed the potent ?-glucosidase inhibitory activity compared with acarbose as a standard material.
Amongst, the compounds 4h and 4i showed the strongest enzyme inhibitory potentials than the standard drug acarbose. There
was a good correlation between in vitro and in silico studies for ligands 4i and 4l. The majority of compounds presented a good
radical scavenging activity, though the compound 4j exhibited the strongest activity, even to the standard of ascorbic acid.
Further studies are required to determine whether these main compounds could be a potential treatment for diabetes and
hyperlipidemia diseases.
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