Synthesis of isoxazole-containing sulfonamides with potent carbonic anhydrase II and VII inhibitory properties

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dc.authorid0000-0003-3342-702Xen_US
dc.authorid0000-0001-9647-7089en_US
dc.authorid0000-0003-4740-1138
dc.contributor.authorAltuğ, Cevher
dc.contributor.authorGüneş, Hanife
dc.contributor.authorNocentini, Alessio
dc.contributor.authorMonti, Simona Maria
dc.contributor.authorBuonanno, Martina
dc.date.accessioned2021-06-23T19:48:59Z
dc.date.available2021-06-23T19:48:59Z
dc.date.issued2017
dc.departmentBAİBÜ, Fen Edebiyat Fakültesi, Kimya Bölümüen_US
dc.description.abstractTwo series of benzenesulfonamide containing isoxazole compounds were prepared by using conventional and microwave (MW) methods. 5-Amino-3-aryl-N-(4-sulfamoylphenyl)isoxazole-4-carboxamide derivatives were synthesized by the reaction of hydroxymoyl chlorides with 2-cyano-N-(4-sulfamoylphenyl)acetamide in the presence of triethylamine. The synthesized 5-amino isoxazoles were reacted with various benzoyl chlorides in order to obtain 5-amidoisoxazoles. The novel compounds were screened in vitro as inhibitors of four human (h) isoforms of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1): hCA I, hCA II, hCA IV and hCA VII. The derivatives of the first series were shown to possess excellent inhibitory activity against the cytosolic isoform hCA II, an antiglaucoma drug target, with Kis in the range of 0.5-49.3 nM and hCA VII, a recently validated anti-neuropathic pain target with Kis in the range of 4.3-51.9 nM. (C) 2017 Elsevier Ltd. All rights reserved.en_US
dc.identifier.doi10.1016/j.bmc.2017.01.008
dc.identifier.endpage1464en_US
dc.identifier.issn0968-0896
dc.identifier.issn1464-3391
dc.identifier.issue4en_US
dc.identifier.pmid28111158en_US
dc.identifier.scopus2-s2.0-85009754069en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.startpage1456en_US
dc.identifier.urihttps://doi.org/10.1016/j.bmc.2017.01.008
dc.identifier.urihttps://hdl.handle.net/20.500.12491/9295
dc.identifier.volume25en_US
dc.identifier.wosWOS:000394632100017en_US
dc.identifier.wosqualityQ2en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.institutionauthorAltuğ, Cevher
dc.institutionauthorGüneş, Hanife
dc.language.isoenen_US
dc.publisherPergamon-Elsevier Science Ltden_US
dc.relation.ispartofBioorganic & Medicinal Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subject5-Amino Isoxazoleen_US
dc.subject5-Amidoisoxazoleen_US
dc.subjectCarbonic Anhydraseen_US
dc.subjectSulfonamideen_US
dc.subjectAmideen_US
dc.titleSynthesis of isoxazole-containing sulfonamides with potent carbonic anhydrase II and VII inhibitory propertiesen_US
dc.typeArticleen_US

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