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  • MakaleYalnız künye2014
    Synthesis and carbonic anhydrase inhibitory effects of novel sulfamides derived from 1-aminoindanes and anilines

    Akbaba, Yusuf; Bastem, Enes; Topal, Fevzi; Gülçin, Ilhami; Marasç, Ahmet; Göksu, Süleyman

    Three 1-aminoindanes, four anilines and BnOH or t-BuOH were reacted with chlorosulfonyl isocyanate to give sulfamoyl carbamates. Pd-C catalysed hydrogenolysis reactions of carbamates or deprotection of the Boc group of the carbamates with CF3CO2H afforded seven novel sulfamides. Human carbonic anhydrase (hCA) isoenzymes I and II (hCA I and hCA II) were purified from fresh human blood erythrocytes with onestep affinity chromatography on Sepharose 4B-tyrosine-sulfanilamide. The inhibitory properties of the novel sulfamides on both isoenzymes were determined using the esterase activity with 4-nitrophenyl acetate (NPA) as substrate. The tested novel sulfamides derived from 1-aminoindanes and anilines effectively inhibited hCA I and II competitively in the nanomolar range. Among these compounds, the novel sulfamide derivative 17 showed themost potent inhibitory effect against hCA I (Ki: 153.88 nM), while sulfamide derivative 26 showed the highest inhibitory potential against hCA II (Ki: 117.80nM).

    • SDG 3 · Sağlık ve Kaliteli Yaşam
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AlanDeğerDil
dc.date.accessioned2026-10-22T10:24:08.550162712Z
dc.date.available2026-10-22T10:24:08.550162712Z
dc.identifier.urihttps://rdlopen.rawdatalibrary.net/r/gumushane/15525
dc.rightsinfo:eu-repo/semantics/openAccess
dc.titleBastem, Enes
dspace.entity.typePerson
person.affiliation.nameDepartment of Medical Services and Techniques, Vocational School of Health Services, Gumushane University Gumushane, Türkiye
person.familyNameBastem
person.givenNameEnes
person.identifier.scopus56437719900
person.statusunverified