title: Synthesis and carbonic anhydrase inhibitory activities of new thienyl-substituted pyrazoline benzenesulfonamides.
abstract: A series of new thienyl-substituted pyrazoline benzenesulfonamides were synthesized and their carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activities were tested on the human (h) isoforms hCA I and hCA II. The inhibition constant (Ki) of these sulfonamides were in the range of 232.16-637.70 nM toward the slow cytosolic isozyme hCA I, and in the range of 342.07-455.80 nM toward hCA II. Many of these compounds showed comparable inhibition with the reference sulfonamide acetazolamide, a clinically used drug. As the sulfonamide CA inhibitors (CAIs) show many therapeutic uses, these derivatives represent interesting examples of a novel class of such derivatives.
authors.affiliation: a Department of Chemistry , Faculty of Science, Ataturk University , Erzurum , Turkey.
authors.forename: Ebru
authors.initials: E
authors.lastname: Mete
authors.affiliation: b Department of Pharmaceutical Chemistry , Faculty of Pharmacy, Ataturk University , Erzurum , Turkey.
authors.forename: Birnur
authors.initials: B
authors.lastname: Comez
authors.affiliation: b Department of Pharmaceutical Chemistry , Faculty of Pharmacy, Ataturk University , Erzurum , Turkey.
authors.forename: Halise
authors.initials: H
authors.lastname: Inci Gul
authors.affiliation: a Department of Chemistry , Faculty of Science, Ataturk University , Erzurum , Turkey.|c Department of Zoology , College of Science, King Saud University , Riyadh , Saudi Arabia , and.
authors.forename: Ilhami
authors.initials: I
authors.lastname: Gulcin
authors.affiliation: d Neurofarba Department and Laboratorio di Chimica Bioinorganica, Polo Scientifico, Universita' degli Studi di Firenze , Sesto Fiorentino (Firenze) , 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; D007527:Isoenzymes / Q000037:antagonists & inhibitors / Q000378:metabolism; D015394:Molecular Structure; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000096926:Benzenesulfonamides
chemical_list: D024401:Carbonic Anhydrase I; D024402:Carbonic Anhydrase II; D002257:Carbonic Anhydrase Inhibitors; D007527:Isoenzymes; D011720:Pyrazoles; D013449:Sulfonamides; D000096926:Benzenesulfonamides
keywords: Benzenesulfonamides; carbonic anhydrase; pyrazoline; synthesis; thiophene