title: Synthesis, characterization and carbonic anhydrase inhibitory activity of novel benzothiazole derivatives.
abstract: N-protected amino acids were reacted with substituted benzothiazoles to give the corresponding N-protected amino acid-benzothiazole conjugates (60-89%). Their structures were confirmed by proton nuclear magnetic resonance ((1)H NMR), carbon-13 nuclear magnetic resonance ((13)C NMR), IR and elemental analysis. Their carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activities were determined against two cytosolic human isoforms (hCA I and hCA II), one membrane-associated (hCA IV) and one transmembrane (hCA XII) enzyme by a stopped-flow CO2 hydrase assay method. The new compounds showed rather weak, micromolar inhibitory activity against most of these enzymes.
authors.affiliation: a Department of Basic Pharmaceutical Sciences , Faculty of Pharmacy, İnönü University , Malatya , Turkey .|b Laboratoria Di Chimica Bioinorganica , Universitâ Degli Studi Di Firenze , Firenze , Italy , and.
authors.forename: F Zehra
authors.initials: FZ
authors.lastname: Küçükbay
authors.affiliation: c Department of Chemistry , Faculty of Arts and Science, İnönü University , Malatya , Turkey.
authors.forename: Nesrin
authors.initials: N
authors.lastname: Buğday
authors.affiliation: b Laboratoria Di Chimica Bioinorganica , Universitâ Degli Studi Di Firenze , Firenze , Italy , and.|c Department of Chemistry , Faculty of Arts and Science, İnönü University , Malatya , Turkey.
authors.forename: Hasan
authors.initials: H
authors.lastname: Küçükbay
authors.affiliation: b Laboratoria Di Chimica Bioinorganica , Universitâ Degli Studi Di Firenze , Firenze , Italy , and.
authors.forename: Muhammet
authors.initials: M
authors.lastname: Tanc
authors.affiliation: b Laboratoria Di Chimica Bioinorganica , Universitâ Degli Studi Di Firenze , Firenze , Italy , and.
authors.forename: Claudiu T
authors.initials: CT
authors.lastname: Supuran
mesh_terms: D052160:Benzothiazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D066241:Carbon-13 Magnetic Resonance Spectroscopy; D002257:Carbonic Anhydrase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D066244:Proton Magnetic Resonance Spectroscopy
chemical_list: D052160:Benzothiazoles; D002257:Carbonic Anhydrase Inhibitors
keywords: Amino acid-benzothiazole conjugates; benzothiazole; carbonic anhydrase