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dc.contributor.authorGuzel-Akdemir, Ozlen; Akdemir, Atilla; Pan, Peiwen; Vermelho, Alane B.; Parkkila, Seppo; Scozzafava, Andrea; Capasso, Clemente; Supuran, Claudiu T.
dc.date.accessioned2021-03-14T19:17:51Z
dc.date.available2021-03-14T19:17:51Z
dc.date.issued01.07.2013
dc.identifier.issn0022-2623
dc.identifier.urihttp://hdl.handle.net/20.500.12645/28527
dc.description.abstractTrypanosoma cruzi, the causative agent of Chagas disease, encodes for an alpha-carbonic anhydrase (CA, EC 4.2.1.1) possessing high catalytic activity (TcCA) which was recently characterized (Pan et al. J. Med. Chem. 2013, 56, 1761-1771). A new class of sulfonamides possessing low nanomolar/subnanomolar TcCA inhibitory activity is described here. Aromatic/heterocydic sulfonamides incorporating halogeno/methoxyphenacetamido tails inhibited TcCA with K(I)s in the range of 0.5-12.5 nM, being less effective against the human off-target isoforms hCA I and II. A homology model of TcCA helped us to rationalize the excellent inhibition profile of these compounds against the protozoan enzyme, a putative new antitrypanosoma drug target. These compounds were ineffective antitrypanosomal agents in vivo due to penetrability problems of these highly polar molecules that possess sulfonamide moieties.
dc.language.isoen
dc.subjectAnatomy; Nasal Cavity; Nasal Sinuses; Turbinates; Computed Tomography
dc.titleA Class of Sulfonamides with Strong Inhibitory Action against the alpha-Carbonic Anhydrase from Trypanosoma cruzi
dc.typeArticle
dc.identifier.wosWOS:000322503000011
dc.identifier.doi10.1021/jm400418p
dc.identifier.pubmed23815159
dc.identifier.eissn1520-4804


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