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Bu çalışmada, yeni 1,2,3-triazol bileşiklerinin (4 ve 5) sentezi, karakterizasyonu, ksantin oksidaz enzimi üzerine in vitro inhibisyon etkilerinin incelenmesi ve moleküler doking çalışmaları gerçekleştirildi. Bu amaçla öncelikle; hedef ürünler (4 ve 5), bütadien sülfondan çıkılarak çeşitli kimyasal transformasyonlarla sentezlendi. Sentezlenen bütün bileşiklerin yapıları spektroskopik yöntemlerle aydınlatıldı. İkinci aşamada; 4 ve 5 bileşiklerinin ksantin oksidaz enzimi üzerine in vitro inhibisyon etkileri incelendi. Enzim inhibisyon sonuçlarına göre; 4 (IC50 = 0.609 µM) ve 5 (IC50 = 0.901 µM) bileşiklerinin, ksantin oksidaz enzim inhibisyonu için ilaç olarak kullanılan Allopurinol’den (IC50 = 1.143 µM) daha güçlü inhibisyon etki gösterdiği tespit edildi. Son olarak; 4 ve 5 bileşiklerinin, ksantin oksidaz eziminin (PDB ID:3NVY) aktif kısmına bağlanma modları, moleküler doking çalışmaları ile açıklandı.
In this study, the synthesis, characterization of new 1,2,3-triazol compounds (4 and 5) and in vitro inhibition effects on xanthin oxidase enzyme were studied and molecular tissue studies were conducted. For this purpose, first and foremost; target products (4 and 5) were synthesized with various chemical transformations by extracting from the butadian sulfate. The structures of all the synthesized compounds were illuminated by spectroscopic methods. In the second stage, the in vitro inhibition effects of the 4 and 5 compounds on the enzyme xanthin oxidase were studied. According to the enzyme inhibition results; 4 (IC50 = 0.609 μM) and 5 (IC50 = 0.901 μM) compounds were found to have a stronger inhibition effect than Allopurinol (IC50 = 1.143 μM) used as a drug for xanthin oxidase enzyme inhibition. Finally, the modes of linking the 4 and 5 compounds to the active part of xanthenic oxidase (PDB ID:3NVY) were explained by molecular tissue studies.
In this study, the synthesis, characterization of novel 1,2,3-triazole compounds (4 and 5), investigation of their in vitro inhibition effects on xanthine oxidase and molecular docking studies were carried out. For this purpose, firstly; the target products (4 and 5) were synthesized by various chemical transformations starting from butadiene sulfone. All of the synthesized compounds were characterized by spectroscopic methods. In the second step; in vitro inhibition effects of compounds 4 and 5 on xanthine oxidase were investigated. According to the enzyme inhibition results, It was determined that compounds 4 (IC50 = 0.609 µM) and 5 (IC50 = 0.901 µM) showed stronger inhibition effect than allopurinol (IC50 = 1.143 µM), which is used as a drug for inhibition of xanthine oxidase. Finally, the binding modes of compounds 4 and 5 in the active part of xanthine oxidase (PDB ID:3NVY) were explained by molecular docking studies.
Alan : Fen Bilimleri ve Matematik; Mühendislik
Dergi Türü : Ulusal
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