title: The effects of some bromophenols on human carbonic anhydrase isoenzymes.
abstract: Carbonic anhydrases (CAs, EC 4.2.1.1), which are involved in a variety of physiological and pathological processes, are ubiquitous metalloenzymes mainly catalyzing the reversible hydration of carbon dioxide (CO2) to bicarbonate ([Formula: see text]) and proton (H(+)). In this study, a dozen of bromophenol derivatives (1-12) were evaluated as metalloenzyme CA (EC 4.2.1.1) inhibitors against the human carbonic anhydrase isoenzymes I and II (hCA I and II). Cytosolic hCA I and II isoenzymes were effectively inhibited by bromophenol derivatives (1-12) with Kis in the low nanomolar range of 1.85 ± 0.58 to 5.04 ± 1.46 nM against hCA I and in the range of 2.01 ± 0.52 to 2.94 ± 1.31 nM against hCA II, respectively.
authors.affiliation: a Department of Chemistry , Faculty of Science, Atatürk University , Erzurum , Turkey .
authors.forename: Parham
authors.initials: P
authors.lastname: Taslimi
authors.affiliation: a Department of Chemistry , Faculty of Science, Atatürk University , Erzurum , Turkey .|b Department of Zoology , College of Science, King Saud University , Riyadh , Saudi Arabia .
authors.forename: İlhami
authors.initials: İ
authors.lastname: Gülçin
authors.affiliation: a Department of Chemistry , Faculty of Science, Atatürk University , Erzurum , Turkey .
authors.forename: Necla
authors.initials: N
authors.lastname: Öztaşkın
authors.affiliation: c Department of Food Technology , Oltu Vocational School, Atatürk University , Oltu , Erzurum , Turkey .
authors.forename: Yasin
authors.initials: Y
authors.lastname: Çetinkaya
authors.affiliation: a Department of Chemistry , Faculty of Science, Atatürk University , Erzurum , Turkey .
authors.forename: Süleyman
authors.initials: S
authors.lastname: Göksu
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 , Universita degli Studi di Firenze , Sesto Fiorentino , Firenze , Italy , and.|e Section of Pharmaceutical and Nutriceutical Sciences, Neurofarba Department, Universita 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 / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D015394:Molecular Structure; D010636:Phenols / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D010636:Phenols; D024401:Carbonic Anhydrase I; D024402:Carbonic Anhydrase II
keywords: Bromophenols; carbonic anhydrase; enzyme inhibition; enzyme purification; isoenzymes