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Chromene-Containing Aromatic Sulfonamides with Carbonic Anhydrase Inhibitory Properties

Andrea Angeli, В. Г. Карцев, Anthi Petrou, Mariana Pinteală, В. С. Броварец, Sergii Slyvchuk, Stepan Pilyo, Athina Geronikaki, Claudiu T. Supuran

2021International Journal of Molecular Sciences15 citationsDOIOpen Access PDF

Abstract

hydration in all living organisms, being actively involved in the regulation of a plethora of patho/physiological conditions. A series of chromene-based sulfonamides were synthesized and tested as possible CA inhibitors. Their inhibitory activity was assessed against the cytosolic human isoforms hCA I, hCA II and the transmembrane hCA IX and XII. Several of the investigated derivatives showed interesting inhibition activity towards the tumor associate isoforms hCA IX and hCA XII. Furthermore, computational procedures were used to investigate the binding mode of this class of compounds, within the active site of hCA IX.

Topics & Concepts

Carbonic anhydraseGene isoformChemistryCytosolInhibitory postsynaptic potentialBiochemistryEnzymeTransmembrane proteinCarbonic Anhydrase IActive siteIsozymeStereochemistryBiologyReceptorGeneNeuroscienceEnzyme function and inhibitionSynthesis and Catalytic ReactionsCholinesterase and Neurodegenerative Diseases
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