TY - JOUR
T1 - Carbonic anhydrase inhibitors; Phosphoryl-sulfonamides - A new class of high affinity inhibitors of isozymes I and II
AU - Fenesan, Ioan
AU - Popescu, Rodica
AU - Scozzafava, Andrea
AU - Crucin, Viorica
AU - Mateiciuc, Elena
AU - Bauer, Roland
AU - Ilies, Marc A.
AU - Supuran, Claudiu T.
PY - 2000
Y1 - 2000
N2 - 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.
AB - 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.
KW - Carbonic Anhydrase Inhibitors/pharmacology
KW - Carbonic Anhydrases/drug effects
KW - Catalytic Domain/drug effects
KW - Humans
KW - Isoenzymes/antagonists & inhibitors
KW - Organophosphates/pharmacology
KW - Recombinant Proteins/drug effects
KW - Structure-Activity Relationship
KW - Sulfonamides/pharmacology
UR - http://www.scopus.com/inward/record.url?scp=0034036657&partnerID=8YFLogxK
U2 - 10.3109/14756360009040690
DO - 10.3109/14756360009040690
M3 - Article
C2 - 10811034
AN - SCOPUS:0034036657
SN - 8755-5093
VL - 15
SP - 297
EP - 309
JO - Journal of Enzyme Inhibition
JF - Journal of Enzyme Inhibition
IS - 3
ER -