0000000001305889

AUTHOR

Daniel R. Vega

showing 2 related works from this author

Salts of 5-amino-2-sulfonamide-1,3,4-thiadiazole, a structural and analog of acetazolamide, show interesting carbonic anhydrase inhibitory properties…

2015

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.

medicine.medical_treatmentPharmacology01 natural sciencesIsozymeThiadiazolesCarbonic anhydraseThiadiazolesDrug DiscoverymedicineHumansCarbonic Anhydrase InhibitorsDiureticsPharmacologySulfonamidesbiology010405 organic chemistryChemistrySulfonamide (medicine)NeurotoxicityGeneral Medicinemedicine.disease0104 chemical sciencesAcetazolamideIsoenzymes010404 medicinal & biomolecular chemistryAnticonvulsantbiology.proteinAnticonvulsantsDiureticAcetazolamidemedicine.drug
researchProduct

CCDC 730598: Experimental Crystal Structure Determination

2017

Related Article: Jorge R. A. Diaz, Gerardo Enrique Cami, Malva Liu-Gonzalez, Daniel R. Vega, Daniela Vullo, Americo Juarez, Jose C. Pedregosa and Claudiu T. Supuran|2016|J.Enzyme Inhib.Med.Chem.|31|1102|doi:10.3109/14756366.2015.1096270

Space GroupCrystallographyCrystal System4-methylbenzene-1-sulfonic acid 5-amino-134-thiadiazole-2-sulfonamideCrystal StructureCell ParametersExperimental 3D Coordinates
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