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Fibrate-based N-acylsulphonamides targeting carbonic anhydrases: synthesis, biochemical evaluation, and docking studies.

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dc.contributor.authorGIAMPIETRO, L
dc.contributor.authorAMMAZZALORSO, A
dc.contributor.authorCARRADORI, S
dc.contributor.authorANGELI, A
dc.contributor.authorDe, Filippis
dc.contributor.authorFANTACUZZI, M
dc.contributor.authorMACCALLINI, C
dc.contributor.authorAkdemir, ATİLLA
dc.contributor.authorSUPURAN, CT
dc.contributor.authorAMOROSO, R
dc.contributor.institutionauthorAKDEMİR, ATİLLA
dc.date.accessioned2019-10-05T12:42:34Z
dc.date.available2019-10-05T12:42:34Z
dc.date.issued2019-12-01
dc.description.abstractA large library of fibrate-based N-acylsulphonamides was designed, synthesised, and fully characterised in order to propose them as zinc binders for the inhibition of human carbonic anhydrase (hCA) enzymatic activity. Synthesised compounds were tested against four hCAs (I, II, IX, and XII) revealing a promising submicromolar inhibitory activity characterised by an isozyme selectivity pattern. Structural modifications explored within this scaffold are: presence of an aryl ring on the sulphonamide, p-substitution of this aryl ring, benzothiazole or benzophenone as core nuclei, and an n-propyl chain or a geminal dimethyl at Ca carbon. Biological results fitted well with molecular modelling analyses, revealing a putative direct interaction with the zinc ion in the active site of hCA I, II and IX. These findings supported the exploration of less investigated secondary sulphonamides as potential hCA inhibitors.en
dc.identifier.citationAMMAZZALORSO A., CARRADORI S., ANGELI A., Akdemir A., De F., FANTACUZZI M., GIAMPIETRO L., MACCALLINI C., AMOROSO R., SUPURAN C., -Fibrate-based N-acylsulphonamides targeting carbonic anhydrases: synthesis, biochemical evaluation, and docking studies.-, Journal of enzyme inhibition and medicinal chemistry, cilt.34, ss.1051-1061, 2019
dc.identifier.doi10.1080/14756366.2019.1611801
dc.identifier.pubmed31074307
dc.identifier.scopus85065774356
dc.identifier.urihttps://hdl.handle.net/20.500.12645/364
dc.identifier.urihttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC6522927/
dc.identifier.wosWOS:000467710900001
dc.language.isoen
dc.rightsinfo:eu-repo/semantics/openAccessen
dc.subjectN-acylsulphonamides
dc.subjectPPAR antagonist
dc.subjectBenzophenone
dc.subjectBenzothiazole
dc.subjectCarbonic anhydrase
dc.subjectFibrate derivatives
dc.titleFibrate-based N-acylsulphonamides targeting carbonic anhydrases: synthesis, biochemical evaluation, and docking studies.
dc.typeArticle
dspace.entity.typePublication
local.article.journalnameJOURNAL OF NEUROSURGERY
local.avesis.id058b460b-5b9d-4007-b93a-77fab2c21db9
local.avesis.response234
local.publication.isinternational1
relation.isAuthorOfPublication19bc513a-c695-4e72-ba1d-83b8d6c574c8
relation.isAuthorOfPublication.latestForDiscovery19bc513a-c695-4e72-ba1d-83b8d6c574c8
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