Cholinesterases, α-Glycosidase, and Carbonic Anhydrase Inhibition Properties of 1H-Pyrazolo[1,2-b]phthalazine-5,10-dione Derivatives: Synthetic Analogues for the Treatment of Alzheimer's Disease and Diabetes Mellitus
2020
Abstract In this study, using the Cu(OTf)2 catalyst, 1H-pyrazolo[1,2-b]phthalazine-5,10-dione derivative molecules were carried out in one step and with high yield (86-91%). The previously synthesized 1H-pyrazolo[1,2-b]phthalazine-5,10-dione derivative molecules, carbonic anhydrase I and II isozymes (hCA I and II), acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and α-glycosidase (α-Gly) enzyme with Ki values in the range of 4.88-15.94 nM for hCA I, 7.04-20.83 nM for hCA II, 68.25-158.27 for AChE, 60.17-91.27 for BChE and 0.36-2.36 nM for α-Gly, respectively. In silico studies were performed on the molecules inhibiting hCA I, hCA II, AChE, BChE and α-Gly receptors. When we evaluated the data obtained in this work, we determined the inhibition type of the 1H-pyrazolo[1,2-b]phthalazine-5,10-dione derivative compounds at the receptors. Reference inhibitors were used for all enzymes.
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