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dc.contributor.authorDemir-Yazıcı, K
dc.contributor.authorAkdemir, Atilla
dc.contributor.authorSupuran, Ct
dc.contributor.authorAngeli, A
dc.contributor.authorGüzel-Akdemir, Ö
dc.date.accessioned2020-05-20T20:59:11Z
dc.date.available2020-05-20T20:59:11Z
dc.date.issued2020-04-29T00:00:00Z
dc.identifier.urihttps://hdl.handle.net/20.500.12645/17995
dc.description.abstractDue to the increasing resistance of currently used antimicrobial drugs, there is an urgent problem for the treatment of cholera disease, selective inhibition of the α-class carbonic anhydrases (CA, EC 4.2.1.1) from the pathogenic bacterium Vibrio cholerae (VcCA) presents an alternative therapeutic target. In this study, a series of hydrazone derivatives, carrying the 2-(hydrazinocarbonyl)-3-phenyl-1H-indole-5-sulfonamide scaffold, have been evaluated as inhibitors of the VcCA with molecular modeling studies. The results suggest that these compounds may bind to the active site of VcCA. To verify this, VcCA enzyme inhibition studies were performed and as predicted most of the tested compounds displayed potent inhibitory activities against VcCA with three compounds showing KI values lower than 30 nM. In addition, all these compounds showed selectivity for VcCA and the off-targets hCA I and II.en
dc.language.isoen
dc.rightsinfo:eu-repo/semantics/openAccessen
dc.subjectDemir-Yazıcı K., Güzel-Akdemir Ö., Angeli A., Supuran C., Akdemir A., -Novel Indole-Based Hydrazones as Potent Inhibitors of the α-class Carbonic Anhydrase from Pathogenic Bacterium <i>Vibrio cholerae</i>.-, International journal of molecular sciences, cilt.21, 2020
dc.titleNovel Indole-Based Hydrazones as Potent Inhibitors of the α-class Carbonic Anhydrase from Pathogenic Bacterium <i>Vibrio cholerae</i>.
dc.typeArticle
dc.identifier.scopus85084277004
dc.identifier.doi10.3390/ijms21093131
dc.identifier.pubmed32365482
local.publication.isinternational1


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