Journal
BIOORGANIC CHEMISTRY
Volume 97, Issue -, Pages -Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2020.103647
Keywords
1H-pyrazolo[1, 2-b]phthalazine-5; 10-dione; Cholinesterase; Carbonic anhydrase; alpha-glycosidase; Molecular docking
Funding
- Yildiz Technical University Research Fund [2012-01-02-GEP01]
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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 derivatives, carbonic anhydrase I and II isozymes (hCA I and II), acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and alpha-glycosidase (alpha-Gly) enzymes with K-i 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 alpha-Gly, respectively. In silico studies were performed on the molecules inhibiting hCA I, hCA II, AChE, BChE and alpha-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 derivatives at the receptors. Reference inhibitors were used for all enzymes.
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