Carbonic anhydrase inhibitors. Inhibition studies of a coral secretory isoform by sulfonamides.

Article Details


Bertucci A, Innocenti A, Zoccola D, Scozzafava A, Tambutte S, Supuran CT

Carbonic anhydrase inhibitors. Inhibition studies of a coral secretory isoform by sulfonamides.

Bioorg Med Chem. 2009 Jul 15;17(14):5054-8. doi: 10.1016/j.bmc.2009.05.063. Epub 2009 May 30.

PubMed ID
19520577 [ View in PubMed

The inhibition of a newly cloned coral carbonic anhydrase (CA, EC has been investigated with a series of sulfonamides, including some clinically used derivatives (acetazolamide, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, brinzolamide, benzolamide, and sulpiride, or indisulam, a compound in clinical development as antitumor drug), as well as the sulfamate antiepileptic topiramate. Some simple amino-/hydrazine-/hydroxy-substituted aromatic/heterocyclic sulfonamides have also been included in the study. All types of activity have been detected, with low potency inhibitors (K(I)s in the range of 163-770nM), or with medium potency inhibitors (K(I)s in the range of 75.1-105nM), whereas ethoxzolamide, several clinically used sulfonamides and heterocyclic compounds showed stronger potency, with K(I)s in the range of 16-48.2nM. These inhibitors may be useful to better understand the physiological role of the Stylophora pistillata CA (STPCA) in corals and its involvement in biomineralisation in this era of global warming.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
EthoxzolamideCarbonic anhydrase 1ProteinHumans
Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
3-[4-(AMINOSULFONYL)PHENYL]PROPANOIC ACIDCarbonic anhydrase 1Ki (nM)6690N/AN/ADetails
3-[4-(AMINOSULFONYL)PHENYL]PROPANOIC ACIDCarbonic anhydrase 2Ki (nM)495N/AN/ADetails
4-(2-AMINOETHYL)BENZENESULFONAMIDECarbonic anhydrase 2Ki (nM)160N/AN/ADetails
5-[(phenylsulfonyl)amino]-1,3,4-thiadiazole-2-sulfonamideCarbonic anhydrase 2Ki (nM)9N/AN/ADetails
AcetazolamideCarbonic anhydrase 1Ki (nM)250N/AN/ADetails
AcetazolamideCarbonic anhydrase 2Ki (nM)12N/AN/ADetails
BrinzolamideCarbonic anhydrase 1Ki (nM)45000N/AN/ADetails
BrinzolamideCarbonic anhydrase 2Ki (nM)3N/AN/ADetails
CelecoxibCarbonic anhydrase 2Ki (nM)21N/AN/ADetails
DiclofenamideCarbonic anhydrase 1Ki (nM)1200N/AN/ADetails
DiclofenamideCarbonic anhydrase 2Ki (nM)38N/AN/ADetails
DorzolamideCarbonic anhydrase 1Ki (nM)50000N/AN/ADetails
DorzolamideCarbonic anhydrase 2Ki (nM)9N/AN/ADetails
EthoxzolamideCarbonic anhydrase 1Ki (nM)25N/AN/ADetails
EthoxzolamideCarbonic anhydrase 2Ki (nM)8N/AN/ADetails
SulpirideCarbonic anhydrase 2Ki (nM)40N/AN/ADetails
SulthiameCarbonic anhydrase 2Ki (nM)9N/AN/ADetails
TopiramateCarbonic anhydrase 1Ki (nM)250N/AN/ADetails
TopiramateCarbonic anhydrase 2Ki (nM)10N/AN/ADetails
ValdecoxibCarbonic anhydrase 2Ki (nM)43N/AN/ADetails
ZonisamideCarbonic anhydrase 1Ki (nM)56N/AN/ADetails
ZonisamideCarbonic anhydrase 2Ki (nM)35N/AN/ADetails