Three new aromatic sulfonamide inhibitors of carbonic anhydrases I, II, IV and XII

4-Sulfamoyl-N-(3-morpholinopropyl)benzamide (I-1), N-(3-morpholinopropyl)benzene-1,4-disulfonamide (I-2) and N-(4-diethylaminoethoxybenzyl)benzene-1,4-bis(sulfonamide (I-3), were prepared and assayed as inhibitors of four carbonic anhydrase (CA) isoenzymes hCA I, hCA II, hCA IV and hCA XII. These co...

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Veröffentlicht in:	Journal of enzyme inhibition and medicinal chemistry 2013-04, Vol.28 (2), p.289-293
Hauptverfasser:	Supuran, C. T., Maresca, A., Gregá, F., Remko, M.
Format:	Artikel
Sprache:	eng
Schlagworte:	Aromatic sulfonamides carbonic anhydrase inhibitors Carbonic Anhydrase Inhibitors - chemical synthesis Carbonic Anhydrase Inhibitors - chemistry Carbonic Anhydrase Inhibitors - pharmacology Carbonic Anhydrases - isolation & purification Carbonic Anhydrases - metabolism Dose-Response Relationship, Drug glaucoma Humans Molecular Structure Protein Isoforms - antagonists & inhibitors Protein Isoforms - isolation & purification Protein Isoforms - metabolism Structure-Activity Relationship Sulfonamides - chemical synthesis Sulfonamides - chemistry Sulfonamides - pharmacology
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Zusammenfassung:	4-Sulfamoyl-N-(3-morpholinopropyl)benzamide (I-1), N-(3-morpholinopropyl)benzene-1,4-disulfonamide (I-2) and N-(4-diethylaminoethoxybenzyl)benzene-1,4-bis(sulfonamide (I-3), were prepared and assayed as inhibitors of four carbonic anhydrase (CA) isoenzymes hCA I, hCA II, hCA IV and hCA XII. These compounds exhibited nanomolar half maximal inhibitory concentration (IC50) ranging from 58 to 740 nmol/L. All three aromatic sulfonamides show different activities for the isoenzymes studied with lowest affinity against isoenzyme hCA XII.
ISSN:	1475-6366 1475-6374
DOI:	10.3109/14756366.2011.649269