title: The human carbonic anhydrase isoenzymes I and II (hCA I and II) inhibition effects of trimethoxyindane derivatives.
abstract: Carbonic anhydrases (CAs, EC 4.2.1.1) had six genetically distinct families described to date in various organisms. There are 16 known CA isoforms in humans. Human CA isoenzymes I and II (hCA I and hCA II) are ubiquitous cytosolic isoforms. Acetylcholine esterase (AChE. EC 3.1.1.7) is a hydrolase that hydrolyzes the neurotransmitter acetylcholine relaying the signal from the nerve. In this study, some trimethoxyindane derivatives were investigated as inhibitors against the cytosolic hCA I and II isoenzymes, and AChE enzyme. Both hCA isozymes were inhibited by trimethoxyindane derivatives in the low nanomolar range. These compounds were good hCA I inhibitors (Kis in the range of 1.66-4.14 nM) and hCA II inhibitors (Kis of 1.37-3.12 nM) and perfect AChE inhibitors (Kis in the range of 1.87-7.53 nM) compared to acetazolamide as CA inhibitor (Ki: 6.76 nM for hCA I and Ki: 5.85 nM for hCA II) and Tacrine as AChE inhibitor (Ki: 7.64 nM).
authors.affiliation: a Department of Chemistry, Faculty of Sciences , Atatürk University , Erzurum , Turkey .
authors.forename: Parham
authors.initials: P
authors.lastname: Taslimi
authors.affiliation: a Department of Chemistry, Faculty of Sciences , Atatürk University , Erzurum , Turkey .|b Department of Zoology, College of Science , King Saud University , Riyadh , Saudi Arabia .
authors.forename: Ilhami
authors.initials: I
authors.lastname: Gulcin
authors.affiliation: a Department of Chemistry, Faculty of Sciences , Atatürk University , Erzurum , Turkey .
authors.forename: Bunyamin
authors.initials: B
authors.lastname: Ozgeris
authors.affiliation: a Department of Chemistry, Faculty of Sciences , Atatürk University , Erzurum , Turkey .
authors.forename: Suleyman
authors.initials: S
authors.lastname: Goksu
authors.affiliation: c Department of Chemistry, Faculty of Science and Arts , Sutcu Imam University , Kahramanmaras , Turkey .
authors.forename: Ferhan
authors.initials: F
authors.lastname: Tumer
authors.affiliation: b Department of Zoology, College of Science , King Saud University , Riyadh , Saudi Arabia .
authors.forename: Saleh H
authors.initials: SH
authors.lastname: Alwasel
authors.affiliation: d Dipartimento di Chimica Ugo Schiff , Università degli Studi di Firenze , Sesto Fiorentino (Firenze) , Italy , and.|e Neurofarba Department, Section of Pharmaceutical and Nutriceutical Sciences , Università degli Studi di Firenze , Sesto Fiorentino (Florence) , Italy.
authors.forename: Claudiu T
authors.initials: CT
authors.lastname: Supuran
mesh_terms: D024401:Carbonic Anhydrase I / Q000037:antagonists & inhibitors* / Q000378:metabolism; D024402:Carbonic Anhydrase II / Q000037:antagonists & inhibitors* / Q000378:metabolism; D002257:Carbonic Anhydrase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007189:Indans / Q000737:chemistry / Q000494:pharmacology*; D007527:Isoenzymes / Q000037:antagonists & inhibitors / Q000378:metabolism; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D007189:Indans; D007527:Isoenzymes; D024401:Carbonic Anhydrase I; D024402:Carbonic Anhydrase II
keywords: Acetylcholine esterase; affinity chromatography carbonic anhydrase; enzyme inhibition; enzyme purification; trimethoxyindane derivatives