6533b82afe1ef96bd128b74c
RESEARCH PRODUCT
X-ray crystallography-promoted drug design of carbonic anhydrase inhibitors.
Jekaterina IvanovaJanis LeitansRaivis ZalubovskisMuhammet TancKaspars TarsKaspars TarsClaudiu T. SupuranAndris Kazakssubject
DrugModels MolecularStereochemistryProtein Conformationmedia_common.quotation_subjectCrystallography X-RayCatalysisHydrolysischemistry.chemical_compoundCarbonic anhydraseMaterials ChemistryHumansCarbonic Anhydrase Inhibitorsmedia_commonCarbonic Anhydraseschemistry.chemical_classificationIsothiazolebiologyMetals and AlloysGeneral ChemistryLyaseSurfaces Coatings and FilmsElectronic Optical and Magnetic MaterialsIsoenzymesEnzymechemistryDrug DesignX-ray crystallographyCeramics and Compositesbiology.proteinSelectivitydescription
1-N-Alkylated-6-sulfamoyl saccharin derivatives were prepared and assayed as carbonic anhydrase inhibitors (CAIs). During X-ray crystallographic experiments an unexpected hydrolysis of the isothiazole ring was evidenced which allowed us to prepare highly potent enzyme inhibitors with selectivity for some isoforms with medical applications.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2015-03-28 | Chemical communications (Cambridge, England) |