title: Synthesis and carbonic anhydrase inhibitory properties of novel coumarin derivatives.
abstract: A newly series of water-soluble 1-alkyl-3-(4-methyl-7, 8-dihydroxy-2H-chromen-2-one) benzimidazolium chloride salts (3a-j) were synthesized and their inhibitory effects on the activity of purified human carbonic anhydrase (hCA) I and II were evaluated. hCA I and II from human erythrocytes were purified by a simple one step procedure by using Sepharose 4B-L-tyrosine-sulphanilamide affinity column. The result showed that all the synthesized compounds were inhibited the CA isoenzymes activity. Among them, 3g and 3j were found to be most active (IC(50) = 22.09 µM and 20.33 µM) for hCA I and hCA II, respectively.
authors.affiliation: Department of Chemistry, Science and Art Faculty, Inonu University, Malatya, Turkey.
authors.forename: Mert Olgun
authors.initials: MO
authors.lastname: Karatas
authors.forename: Bülent
authors.initials: B
authors.lastname: Alici
authors.forename: Umit
authors.initials: U
authors.lastname: Cakir
authors.forename: Engin
authors.initials: E
authors.lastname: Cetinkaya
authors.forename: Dudu
authors.initials: D
authors.lastname: Demir
authors.forename: Adem
authors.initials: A
authors.lastname: Ergün
authors.forename: Nahit
authors.initials: N
authors.lastname: Gençer
authors.forename: Oktay
authors.initials: O
authors.lastname: Arslan
mesh_terms: D002257:Carbonic Anhydrase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002256:Carbonic Anhydrases / Q000302:isolation & purification / Q000378:metabolism*; D003374:Coumarins / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004912:Erythrocytes / Q000201:enzymology; D006801:Humans; D015394:Molecular Structure; D020033:Protein Isoforms / Q000037:antagonists & inhibitors / Q000302:isolation & purification / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D003374:Coumarins; D020033:Protein Isoforms; C030123:coumarin; D002256:Carbonic Anhydrases