title: Antioxidant Activity, Acetylcholinesterase, and Carbonic Anhydrase Inhibitory Properties of Novel Ureas Derived from Phenethylamines.
abstract: A series of ureas derived from phenethylamines were synthesized and evaluated for human carbonic anhydrase (hCA) I and II, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) enzyme inhibitory activities and antioxidant properties. The ureas were synthesized from the reactions of substituted phenethylamines with N,N-dimethylcarbamoyl chloride; then, the synthesized compounds were converted to their corresponding phenolic derivatives via O-demethylation. hCA I and II were effectively inhibited by the newly synthesized compounds, with Kivalues in the range of 0.307-0.432 nM for hCA I and 0.149-0.278 nM for hCA II. On the other hand, the Kiparameters of these compounds for AChE and BChE were determined in the range of 0.129-0.434 and 0.095-0.207 nM, respectively. Phenolic ureas also showed good antioxidant activities.
authors.affiliation: Faculty of Arts and Sciences, Department of Chemistry, Ordu University, Ordu, Turkey.
authors.forename: Kadir
authors.initials: K
authors.lastname: Aksu
authors.affiliation: Faculty of Science, Department of Basic Sciences, Erzurum Technical University, Erzurum, Turkey.|Faculty of Science, Department of Chemistry, Ataturk University, Erzurum, Turkey.
authors.forename: Bünyamin
authors.initials: B
authors.lastname: Özgeriş
authors.affiliation: Faculty of Science, Department of Chemistry, Ataturk University, Erzurum, Turkey.
authors.forename: Parham
authors.initials: P
authors.lastname: Taslimi
authors.affiliation: Faculty of Science, Department of Chemistry, Ataturk University, Erzurum, Turkey.
authors.forename: Ali
authors.initials: A
authors.lastname: Naderi
authors.affiliation: Faculty of Science, Department of Chemistry, Ataturk University, Erzurum, Turkey.|Department of Zoology, College of Science, King Saud University, Riyadh, Saudi Arabia.
authors.forename: İlhami
authors.initials: İ
authors.lastname: Gülçin
authors.affiliation: Faculty of Science, Department of Chemistry, Ataturk University, Erzurum, Turkey.
authors.forename: Süleyman
authors.initials: S
authors.lastname: Göksu
mesh_terms: D000110:Acetylcholinesterase / Q000378:metabolism*; D000975:Antioxidants / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002091:Butyrylcholinesterase / Q000187:drug effects; D024401:Carbonic Anhydrase I / Q000037:antagonists & inhibitors; D024402:Carbonic Anhydrase II / Q000037:antagonists & inhibitors; D002257:Carbonic Anhydrase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007527:Isoenzymes / Q000037:antagonists & inhibitors; D015394:Molecular Structure; D010084:Oxidation-Reduction; D010627:Phenethylamines / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014508:Urea / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000975:Antioxidants; D002257:Carbonic Anhydrase Inhibitors; D002800:Cholinesterase Inhibitors; D007527:Isoenzymes; D010627:Phenethylamines; D014508:Urea; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase; D024401:Carbonic Anhydrase I; D024402:Carbonic Anhydrase II
keywords: Acetylcholinesterase; Butyrylcholinesterase; Carbonic anhydrase; Enzyme inhibition; Urea