title: Synthesis and carbonic anhydrase inhibitory activity of 4-substituted 2-thiophenesulfonamides.
abstract: A series of 4-substituted 2-thiophenesulfonamides was prepared from 3-thiophenecarboxaldehyde using metalation chemistry developed for 3-furaldehyde. Several of these compounds inhibit carbonic anhydrase II in vitro at concentrations of less than 10 nM. In addition, none of these compounds exhibit sensitization potential as determined from in vitro measurement of cysteine reactivity.
authors.affiliation: Department of Chemical Sciences, Allergan Inc., Irvine, California 92715.
authors.forename: J M
authors.initials: JM
authors.lastname: Holmes
authors.forename: G C
authors.initials: GC
authors.lastname: Lee
authors.forename: M
authors.initials: M
authors.lastname: Wijono
authors.forename: R
authors.initials: R
authors.lastname: Weinkam
authors.forename: L A
authors.initials: LA
authors.lastname: Wheeler
authors.forename: M E
authors.initials: ME
authors.lastname: Garst
mesh_terms: D000818:Animals; D002257:Carbonic Anhydrase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D002924:Ciliary Body / Q000201:enzymology; D006801:Humans; D015394:Molecular Structure; D011817:Rabbits; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology; D013876:Thiophenes / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D013449:Sulfonamides; D013876:Thiophenes