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dc.contributor.authorTurker, Yasin; Aslantas, Yusuf; Turker, Yasemin; Akkaya, Mehmet; Ucgun, Taner; Erkan, Melih Engin
dc.date.accessioned2021-03-14T19:17:51Z
dc.date.available2021-03-14T19:17:51Z
dc.date.issued10.10.2013
dc.identifier.issn0167-5273
dc.identifier.urihttp://hdl.handle.net/20.500.12645/28528
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.subjectMitral regurgitation; NYHA class; Pro-adrenomedullin
dc.titleA novel indicator for assessment of mitral regurgitation severity: Pro-adrenomedullin
dc.typeLetter
dc.identifier.wosWOS:000326184400249
dc.identifier.doi10.1016/j.ijcard.2013.04.007
dc.identifier.pubmed23632110
dc.identifier.eissn1874-1754


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