title: Carbonic anhydrase inhibitors; phosphoryl-sulfonamides--a new class of high affinity inhibitors of isozymes I and II.
abstract: A series of phosphorylated aromatic/heterocyclic sulfonamides with the general formula ArSO2NHPO3H2 have been prepared by condensing ArSO2NH2 with phosphorus pentachloride, followed by controlled hydrolysis in the presence of formic acid. The new derivatives generally act as stronger inhibitors of two carbonic anhydrase (CA) isozymes, CA I and CA II, as compared to the parent unsubstituted sulfonamides from which they were obtained. The inhibition mechanism by this new class of CA inhibitors, as well as structure activity correlations for the series of investigated derivatives, are also discussed.
authors.affiliation: Laboratory of Element-Organic Compounds, Institute of Chemistry Raluca Ripan Cluj Napoca, Roumania.
authors.forename: I
authors.initials: I
authors.lastname: Fenesan
authors.forename: R
authors.initials: R
authors.lastname: Popescu
authors.forename: A
authors.initials: A
authors.lastname: Scozzafava
authors.forename: V
authors.initials: V
authors.lastname: Crucin
authors.forename: E
authors.initials: E
authors.lastname: Mateiciuc
authors.forename: R
authors.initials: R
authors.lastname: Bauer
authors.forename: M A
authors.initials: MA
authors.lastname: Ilies
authors.forename: C T
authors.initials: CT
authors.lastname: Supuran
mesh_terms: D002257:Carbonic Anhydrase Inhibitors / Q000494:pharmacology*; D002256:Carbonic Anhydrases / Q000187:drug effects* / Q000235:genetics; D020134:Catalytic Domain / Q000187:drug effects; D006801:Humans; D007527:Isoenzymes / Q000037:antagonists & inhibitors; D010755:Organophosphates / Q000494:pharmacology*; D011994:Recombinant Proteins / Q000187:drug effects; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000494:pharmacology*
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D007527:Isoenzymes; D010755:Organophosphates; D011994:Recombinant Proteins; D013449:Sulfonamides; D002256:Carbonic Anhydrases