title: Spirobisnaphthalenes effectively inhibit carbonic anhydrase.
abstract: This study explores the correlation between human carbonic anhydrase (CA, EC 4.2.1.1) isoforms I and II (hCA I, II) and the inhibitory features of some spirobisnaphthalene derivatives. A group of spirobisnaphthalenes was synthesized and their hCA I and II inhibitory effects was investigated. The Ki values were similar for both CA isoenzymes, the compounds showing good inhibitory activity. Ki values ranged between 1.60 and 460.42 µM for hCA I and between 0.39 and 419.42 µM for hCA II, respectively. The spirobisnaphthalenes derivatives might be useful for designing CA inhibitors belonging to novel chemotypes compared to the highly investigated sulfonamides, sulfamates or coumarins.
authors.affiliation: a Central Researching Laboratory , Agri Ibrahim Cecen University , Agri , Turkey .
authors.forename: Hulya
authors.initials: H
authors.lastname: Gocer
authors.affiliation: b School of Health, Agri Ibrahim Cecen University , Agri , Turkey .
authors.forename: Abdulselam
authors.initials: A
authors.lastname: Aslan
authors.affiliation: c Department of Chemistry, Faculty of Science , Atatürk University , Erzurum , Turkey .|d Zoology Department , College of Science, King Saud University , Riyadh , Saudi Arabia .
authors.forename: İlhami
authors.initials: İ
authors.lastname: Gülçin
authors.affiliation: e Dipartimento di Chimica Ugo Schiff , Universita degli Studi di Firenze , Sesto Fiorentino (Firenze) , Italy , and.|f 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: D002257:Carbonic Anhydrase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002256:Carbonic Anhydrases / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007527:Isoenzymes / Q000037:antagonists & inhibitors / Q000378:metabolism; D015394:Molecular Structure; D009281:Naphthalenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013141:Spiro Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D007527:Isoenzymes; D009281:Naphthalenes; D013141:Spiro Compounds; D002256:Carbonic Anhydrases
keywords: Carbonic anhydrase; enzyme inhibition; enzyme purification; spirobisnaphthalenes