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Novel 2-indolinones containing a sulfonamide moiety as selective inhibitors of candida β-carbonic anhydrase enzyme.

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dc.contributor.advisorInhibition of the b-carbonic anhydrase (CA, EC 4.2.1.1) from pathogenic Candida glabrata (CgNce103) by 1H-indole-2,3-dione 3-[N-(4-sulfamoylphenyl)thiosemicarbazones] 4a–m was investigated. All the compounds were found to be potent inhibitors of CgNce103, with inhibition constants in the range of 6.4- 63.9 nM. The 5,7-dichloro substituted derivative 4l showed the most effective inhibition (KI of 6.4 nM) as well as the highest selectivity for inhibiting CgNce103 over the cytosolic human (h) isoforms hCA I and II. A possible binding interaction of compound 4l within the active site of CgNce103 has been proposed based on docking studies.en
dc.contributor.authorAkdemir, ATİLLA
dc.contributor.authorANGELI, A
dc.contributor.authorGÖKTAŞ, F
dc.contributor.authorEraslan, Elma
dc.contributor.authorKARALı, N
dc.contributor.authorSUPURAN, CT
dc.contributor.institutionauthorAKDEMİR, ATİLLA
dc.date.accessioned2019-10-05T14:24:04Z
dc.date.available2019-10-05T14:24:04Z
dc.date.issued2019-12-01
dc.description.abstractInhibition of the b-carbonic anhydrase (CA, EC 4.2.1.1) from pathogenic Candida glabrata (CgNce103) by 1H-indole-2,3-dione 3-[N-(4-sulfamoylphenyl)thiosemicarbazones] 4a–m was investigated. All the compounds were found to be potent inhibitors of CgNce103, with inhibition constants in the range of 6.4- 63.9 nM. The 5,7-dichloro substituted derivative 4l showed the most effective inhibition (KI of 6.4 nM) as well as the highest selectivity for inhibiting CgNce103 over the cytosolic human (h) isoforms hCA I and II. A possible binding interaction of compound 4l within the active site of CgNce103 has been proposed based on docking studies.en
dc.identifier10.3233/dma-2011-0800
dc.identifier.citationAkdemir A., ANGELI A., GÖKTAŞ F., Eraslan E., KARALı N., SUPURAN C., -Novel 2-indolinones containing a sulfonamide moiety as selective inhibitors of candida β-carbonic anhydrase enzyme.-, Journal of enzyme inhibition and medicinal chemistry, cilt.34, ss.528-531, 2019
dc.identifier.doi10.1080/14756366.2018.1564045
dc.identifier.pubmed30724625
dc.identifier.scopus85061106138
dc.identifier.urihttps://hdl.handle.net/20.500.12645/3777
dc.identifier.wosWOS:000457960800001
dc.language.isoen
dc.rightsinfo:eu-repo/semantics/openAccess
dc.titleNovel 2-indolinones containing a sulfonamide moiety as selective inhibitors of candida β-carbonic anhydrase enzyme.
dc.typeArticle
dspace.entity.typePublication
local.article.journalnameDisease markers
local.avesis.id5b8823c2-4aa0-4e04-85ba-127b77d0d6b0
local.avesis.response3647
local.publication.isinternational1
relation.isAuthorOfPublication19bc513a-c695-4e72-ba1d-83b8d6c574c8
relation.isAuthorOfPublication.latestForDiscovery19bc513a-c695-4e72-ba1d-83b8d6c574c8
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