- In vitro inhibitory effects of some acetophenone derivatives on some metabolic enzymes and molecular docking.
In vitro inhibitory effects of some acetophenone derivatives on some metabolic enzymes and molecular docking.
In this study, the acetophenone derivatives 1-6 were found to be effective inhibitor molecules for ฮฑ-glycosidase, human carbonic anhydrases I and II (hCA I/II), and acetylcholinesterase (AChE), with Ki values in the range of 167.98โยฑโ25.06 to 304.36โยฑโ65.45โยตM for ฮฑ-glycosidase, 555.76โยฑโ56.07 to 1,043.66โยฑโ98.78โยตM for hCA I, 598.63โยฑโ90.04 to 945.76โยฑโ74.50โยตM for hCA II, and 71.34โยฑโ11.25 to 143.75โยฑโ31.27โยตM for AChE, and IC50 values of 73.65-101.13โยตM for tyrosinase. In the last step, molecular docking calculations were performed to compare the biological activities of molecules with their docking scores in these enzymes. The interactions of the studied molecules against human ฮฑ-galactosidase (PDB ID: 1R47), hCA I (PDB ID: 3LXE), human AChE (PDB ID: 4M0E), hCA II (PDB ID: 5AML), and human tyrosinase (PDB ID: 5M8Q) were examined to compare the biological activity values. The ADME/T analysis (adsorption, distribution, metabolism, and discharge) was then performed for the future use of these molecules as drugs.