Background: To discover novel lead molecules against diabetes, Alzheimer's disease and oxidative stress, a library of arylated pyrazole-fused pyran derivatives, 1-20, were synthesized in a one-pot reaction. Materials & methods:(1)H-NMR spectroscopic and electron ionization mass spectrometry techniques were used to characterize the synthetic hybrid molecules 1-20. Analogs were screened against four indispensable therapeutic targets, including alpha-amylase, alpha-glucosidase, acetylcholinesterase and butyrylcholinesterase enzymes. Results: Except for derivatives 17 and 18, all other compounds exhibited varying degrees of inhibitory activities against target enzymes. The kinetic studies revealed that the synthetic molecules followed a competitive-type mode of inhibition for alpha-amylase and acetylcholinesterase enzymes, as well as a non-competitive mode of inhibition for alpha-glucosidase and butyrylcholinesterase enzymes. In addition, molecular docking studies identified crucial binding interactions of ligands with the enzyme's active site. Conclusion: These molecules may serve as a potential drug candidate to cure diabetes, Alzheimer's disease and oxidative stress in the future.
        
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Hameed S, Babatunde O, Salar U, Jabbar A, Chigurupati S, Solangi M, Atta L, Ul-Haq Z, Saleem F, Bhatia S, Al-Harrasi A, Taha M, Khan KM (2022) Efficient one-pot synthesis of arylated pyrazole-fused pyran analogs: as leads to treating diabetes and Alzheimer's disease Future Med Chem
Hameed S, Babatunde O, Salar U, Jabbar A, Chigurupati S, Solangi M, Atta L, Ul-Haq Z, Saleem F, Bhatia S, Al-Harrasi A, Taha M, Khan KM (2022) Future Med Chem