6533b834fe1ef96bd129e23d
RESEARCH PRODUCT
Salts of 5-amino-2-sulfonamide-1,3,4-thiadiazole, a structural and analog of acetazolamide, show interesting carbonic anhydrase inhibitory properties, diuretic, and anticonvulsant action
Claudiu T. SupuranMalva Liu-gonzálezJorge R. A. DíazAmérico JuárezJosé C. PedregosaDaniela VulloGerardo Enrique CamíDaniel R. Vegasubject
medicine.medical_treatmentPharmacology01 natural sciencesIsozymeThiadiazolesCarbonic anhydraseThiadiazolesDrug DiscoverymedicineHumansCarbonic Anhydrase InhibitorsDiureticsPharmacologySulfonamidesbiology010405 organic chemistryChemistrySulfonamide (medicine)NeurotoxicityGeneral Medicinemedicine.disease0104 chemical sciencesAcetazolamideIsoenzymes010404 medicinal & biomolecular chemistryAnticonvulsantbiology.proteinAnticonvulsantsDiureticAcetazolamidemedicine.drugdescription
Three salts of 5-amino-2-sulfonamide-1,3,4-thiadiazole (Hats) were prepared and characterized by physico-chemical methods. The p-toluensulfonate, the methylsulfonate, and the chlorhydrate monohydrate salts of Hats were evaluated as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors (CAIs) and as anticonvulsants and diuretics, since many CAIs are clinically used as pharmacological agents. The three Hats salts exhibited diuretic and anticonvulsant activities with little neurotoxicity. The human (h) isoforms hCA I, II, IV, VII, IX, and XII were inhibited in their micromolar range by these salts, whereas pathogenic beta and gamma CAs showed similar, weak inhibitory profiles.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2015-01-01 |