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Bioorg Chem ; 83: 55-62, 2019 03.
Article in English | MEDLINE | ID: mdl-30342386

ABSTRACT

A new coordination polymer Zn(II) with thiosemicarbazone glyoxalic acid H2GAT was obtained in this study. According to the X-ray diffraction data, the coordination of the Zn(II) ion is carried out by one sulfur atom, in the thiol form, one nitrogen atom of the azomethine group and two oxygen atoms of the carboxylate groups, one of which belongs to neighbouring complex molecule. The oxygen atom of the water molecule completes Zn(II) ion environment to a distorted square-pyramidal structure. The binding of the monomer complex into polimer occurs through the bridge oxygen atom of carboxylate group. This complex is effective inhibitor of the α-glycosidase, butyrylcholinesterase (BChE), cytosolic carbonic anhydrase I and II isoforms (hCA I and II), and acetylcholinesterase enzymes (AChE) enzymes with Ki values of 1.45 ±â€¯0.23 µM for hCA I, 2.04 ±â€¯0.11 µM for hCA II, 3.47 ±â€¯0.88 µM for α-glycosidase, 0.47 ±â€¯0.10 µM for BChE, and 0.58 ±â€¯0.13 µM for AChE, respectively.


Subject(s)
Coordination Complexes/pharmacology , Enzyme Inhibitors/pharmacology , Glyoxylates/pharmacology , Polymers/pharmacology , Thiosemicarbazones/pharmacology , Zinc/pharmacology , Acetylcholinesterase/metabolism , Butyrylcholinesterase/metabolism , Carbonic Anhydrase I/antagonists & inhibitors , Carbonic Anhydrase I/metabolism , Carbonic Anhydrase II/antagonists & inhibitors , Carbonic Anhydrase II/metabolism , Coordination Complexes/chemical synthesis , Coordination Complexes/chemistry , Dose-Response Relationship, Drug , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/chemistry , Glycoside Hydrolases/antagonists & inhibitors , Glycoside Hydrolases/metabolism , Glyoxylates/chemistry , Humans , Molecular Structure , Polymers/chemistry , Structure-Activity Relationship , Thiosemicarbazones/chemistry , Zinc/chemistry
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