Abstract:
Pyrazoline and benzimidazoles derivatives have been widely studied due to their potential applications in the
medicinal field. In this research project, we have hybridized these two heterocyclic systems in the same molecule. A new
series of compounds, 2-((3,5-diaryl-4,5-dihydro-1H-pyrazol-1-yl)methyl)-1H-benzo[d]imidazole (5a-i) were synthesized
through a multistep reaction. In the first step, chalcones 3a-i were prepared by coupling of various acetophenones and
benzaldehydes under alkaline conditions. These chalcones were cyclized with hydrazine hydrate to form a series of
pyrazolines which were finally coupled with 2-chloromethyl-1H-benzimidazole to get a new series of titled hybrid
molecules. The structures of these compounds were elucidated by spectral (1H NMR and 13C NMR) analysis. The antidiabetic potential of these compounds was studied by screening them for their α-glucosidase inhibition activity. The SAR
was established through molecular docking analysis. Compound 5d appeared as effective inhibitor with IC50 = 50.06µM
as compared to reference drug (acarbose) having IC50 = 58.8µM.
