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Design, synthesis and biological activity of selective hCAs inhibitors based on 2-(benzylsulfinyl)benzoic acid scaffold.

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dc.contributor.authorDe, Filippis
dc.contributor.authorRotondi, G
dc.contributor.authorGuglielmi, P
dc.contributor.authorDe, Monte
dc.contributor.authorSecci, D
dc.contributor.authorSupuran, CT
dc.contributor.authorMaccallini, C
dc.contributor.authorAmoroso, R
dc.contributor.authorCirilli, R
dc.contributor.authorAngeli, A
dc.contributor.institutionauthorAKDEMİR, ATİLLA
dc.date.accessioned2019-10-05T21:44:22Z
dc.date.available2019-10-05T21:44:22Z
dc.date.issued2019-12-01
dc.description.abstractA large library of derivatives based on the scaffold of 2-(benzylsulfinyl)benzoic acid were synthesised and tested as atypical inhibitors against four different isoforms of human carbonic anhydrase (hCA I, II, IX and XII, EC 4.2.1.1). The exploration of the chemical space around the main functional groups led to the discovery of selective hCA IX inhibitors in the micromolar/nanomolar range, thus establishing robust structure-activity relationships within this versatile scaffold. HPLC separation of some selected chiral compounds and biological evaluation of the corresponding enantiomers was performed along with molecular modelling studies on the most active derivatives.en
dc.identifier.citationRotondi G., Guglielmi P., Carradori S., Secci D., De M., De F., Maccallini C., Amoroso R., Cirilli R., Akdemir A., et al., -Design, synthesis and biological activity of selective hCAs inhibitors based on 2-(benzylsulfinyl)benzoic acid scaffold.-, Journal of enzyme inhibition and medicinal chemistry, cilt.34, ss.1400-1413, 2019
dc.identifier.doi10.1080/14756366.2019.1651315
dc.identifier.pubmed31401897
dc.identifier.urihttps://hdl.handle.net/20.500.12645/8102
dc.identifier.wosWOS:000480545500001
dc.language.isoen
dc.rightsinfo:eu-repo/semantics/openAccessen
dc.titleDesign, synthesis and biological activity of selective hCAs inhibitors based on 2-(benzylsulfinyl)benzoic acid scaffold.
dc.typeArticle
dspace.entity.typePublication
local.article.journalnameMINERVA ANESTESIOLOGICA
local.avesis.idc9771946-0a47-410e-bd81-02868c88be79
local.avesis.response7978
local.publication.isinternational1
relation.isAuthorOfPublication19bc513a-c695-4e72-ba1d-83b8d6c574c8
relation.isAuthorOfPublication.latestForDiscovery19bc513a-c695-4e72-ba1d-83b8d6c574c8
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