Sülfonamit İçeren Maleamik Asit Türevi ile 2-Aminopiridinin Proton Transfer Tuzu ve Co(II) ve Cu(II) Komplekslerinin Sentezi, Karakterizasyonu ve Karbonik Anhidraz İzoenzimleri Üzerindeki İnhibisyon Özelliklerinin İncelenmesi

Bu çalışmada, ilk olarak 3-aminobenzensülfonilamit (abs) ile maleik anhidritin (mal) tepkimesinden (E)-4-okso-4-(3sülfamoyilfenil)amino)büt-2-enoik asit (Hmabsmal) bileşiği sentezlenmiştir. Daha sonra Hmabsmal bileşiği ile 2aminopiridinin (ap) proton transfer tuzu (1) hazırlanmıştır. Bu maddelerin değişik yöntemlerle Co(II) (2) ve Cu(II) (3 ve 4) geçiş metal kompleksleri sentezlenmiştir. Proton transfer tuzunun yapısı elementel analiz, 1H-NMR, 13C-NMR, FT-IR, UV-Vis metotları ile aydınlatılmıştır. Amorf halde elde edilen geçiş metal komplekslerinin yapıları ise elementel analiz, ICP-OES, FT-IR, UV-Vis, termal analiz, manyetik duyarlılık ve molar iletkenlik sonuçları dikkate alınarak önerilmiştir. Ayrıca, sentezlenen maddelerin insan eritrosit hCA I ve hCA II izoenzimleri üzerindeki inhibisyon etkilerini belirlemek üzere in vitro çalışmalar yapılmıştır. Yeni sentezlenen maddelerin izoenzimlerin esteraz aktivitesini inhibe ettiği, hidrataz aktivitesini ise sadece 3 bileşiğinin inhibe ettiği tespit edilmiştir. Bu maddelerin inhibisyon değerlerinin kontrol bileşiği asetazolamid (AAZ) değerleri ile kıyaslanabilir büyüklükte olduğu tespit edilmiştir

Synthesis and Characterization of Proton Transfer Salt Between Maleamic Acid Derivative Including Sulfonamide Moiety and 2-aminopyridine and Preparation of Their Co(II) and Cu(II) Complexes and Investigation of Inhibition Properties on Carbonic Anhydrase Isoenzymes

In this study, firstly (E)-4-oxo-4-(3-sulfamoylphenylamino)but-2-enoic acid (Hmabsmal) has been synthesized from the reaction between 3-aminobenzenesulfonamide (abs) and maleic anhydride (mal) and secondly, proton transfer salt has been prepared from 2-aminopyridine (ap) and Hmabsmal. Transition metal complexes of these substances, Co(II) (2) and Cu(II) (3 and 4), have been synthesized by different methods. The structure of proton transfer compounds have been proposed by using elemantal analysis, H-NMR, C-NMR, UV-Vis techniques. The structure of amorphous metal complexes have been proposed by using elemantal analysis, ICP-OES, FT-IR, UV-Vis, thermal analysis, magnetic susceptibility and molar conductivity techniques. In addition, in vitro studies have been performed to determine the inhibition effects of synthesized compounds on human erythrocyte hCA I and hCA II isoenzymes. It has been observed that synthesized compounds have affected esterase activities of hCA I and hCA II. But only compound 3 has inhibiton effect on the hydratase activities on the isozymes. Also the inhibition values of these compounds are comparable with the inhibition values of control compound acetazolamide (AAZ)

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