Bazı indol-triazol bileşiklerin sentezi ve karbonik anhidraz enzimi üzerine inhibisyon etkisinin incelenmesi
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Dosyalar
Tarih
2018
Yazarlar
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Necmettin Erbakan Üniversitesi
Erişim Hakkı
info:eu-repo/semantics/openAccess
Özet
Bu tez çalışması kapsamında indol-triazol türevi bileşiklerin sentezlenmesi ve insan karbonik anhidraz I ve II izoformları üzerine inhibisyon etkilerinin incelenmesi amaçlanmıştır. Öncelikle elde edilmesi amaçlanan maddelerin enzim ile teorik bağlanma enerjileri moleküler docking ile hesaplandı. Sonrasında indol-3-propiyonik asit ve tiyokarbohidrazit kondenzasyonundan elde edilen 4-amino-1,2,4-triazol-3-tiyon çekirdeğinin schiff bazı, tiyadiazol, tiyadiazin ve tiyoeter türevleri elde edildi. Sentezlenen bileşiklerin kimyasal yapıları FT-IR, 1H-NMR ve 13C-NMR teknikleri ile karakterize edildi ve karbonik anhidraz enziminin esteraz aktivitesine bakılarak, hCA I ve hCAII üzerine inhibisyon etkileri incelendi. İnhibisyon etkileri IC50 değerleri olarak ifade edildi.
In this thesis, it was aimed to synthesize indole-triazole derivative compounds and investigate their inhibition effects against human carbonic anhydrase I and II isoforms. First of all, theoretical binding energies of intended compounds with enzyme was calculated with molecular docking. After that, Schiff base, thiadiazole, thiadiazine and thioether derivatives of 4-amino-1,2,4-triazole-3-thion scaffold was synthesized, which obtained from condensation of indole-3-propionic acid and thiocarbohydrazide. Chemical structures of synthesized compounds were characterized with FT-IR, 1H-NMR and 13C-NMR techniques and inhibition effects on hCA I and hCAII were determined by the esterase activity of the carbonic anhydrase enzyme. Inhibition effects were expressed as IC50 values.
In this thesis, it was aimed to synthesize indole-triazole derivative compounds and investigate their inhibition effects against human carbonic anhydrase I and II isoforms. First of all, theoretical binding energies of intended compounds with enzyme was calculated with molecular docking. After that, Schiff base, thiadiazole, thiadiazine and thioether derivatives of 4-amino-1,2,4-triazole-3-thion scaffold was synthesized, which obtained from condensation of indole-3-propionic acid and thiocarbohydrazide. Chemical structures of synthesized compounds were characterized with FT-IR, 1H-NMR and 13C-NMR techniques and inhibition effects on hCA I and hCAII were determined by the esterase activity of the carbonic anhydrase enzyme. Inhibition effects were expressed as IC50 values.
Açıklama
Doktora Tezi
Anahtar Kelimeler
Docking, İndol, İnhibisyon, Karbonik Anhidraz, Triazol, Docking, Indole, Inhibition, Carbonic Anhydrase, Triazole
Kaynak
WoS Q Değeri
Scopus Q Değeri
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Sayı
Künye
Sarıgüney, A. B. (2018). Bazı indol-triazol bileşiklerin sentezi ve karbonik anhidraz enzimi üzerine inhibisyon etkisinin incelenmesi. (Yayımlanmamış doktora tezi). Necmettin Erbakan Üniversitesi, Fen Bilimleri Enstitüsü, Makine Mühendisliği Anabilim Dalı, Konya.
