Ksantin Oksidaz İnhibitörü Yeni 1,2,3-Triazol Türevlerinin Sentezi, Karakterizasyonu ve Moleküler Doking Çalışmaları

Yıl: 2020 Cilt: 9 Sayı: 2 Sayfa Aralığı: 644 - 654 Metin Dili: Türkçe İndeks Tarihi: 19-11-2020

Ksantin Oksidaz İnhibitörü Yeni 1,2,3-Triazol Türevlerinin Sentezi, Karakterizasyonu ve Moleküler Doking Çalışmaları

Öz:
Bu çalışmada, yeni 1,2,3-triazol bileşiklerinin (4 ve 5) sentezi, karakterizasyonu, ksantin oksidaz enzimi üzerinein vitro inhibisyon etkilerinin incelenmesi ve moleküler doking çalışmaları gerçekleştirildi. Bu amaçla öncelikle;hedef ürünler (4 ve 5), bütadien sülfondan çıkılarak çeşitli kimyasal transformasyonlarla sentezlendi. Sentezlenenbütün bileşiklerin yapıları spektroskopik yöntemlerle aydınlatıldı. İkinci aşamada; 4 ve 5 bileşiklerinin ksantinoksidaz enzimi üzerine in vitro inhibisyon etkileri incelendi. Enzim inhibisyon sonuçlarına göre 4 (IC50 = 0.609µM) ve 5 (IC50 = 0.901 µM) bileşiklerinin, ksantin oksidaz enzim inhibisyonu için ilaç olarak kullanılanallopurinolden (IC50 = 1.143 µM) daha güçlü inhibisyon etki gösterdiği tespit edildi. Son olarak; 4 ve 5bileşiklerinin, ksantin oksidaz eziminin (PDB ID:3NVY) aktif kısmına bağlanma modları, moleküler dokingçalışmaları ile açıklandı.
Anahtar Kelime:

The Synthesis, Characterization and Molecular Docking Studies of Novel 1,2,3-Triazole Derivatives as Xanthine Oxidase Inhibitor

Öz:
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.
Anahtar Kelime:

Belge Türü: Makale Makale Türü: Araştırma Makalesi Erişim Türü: Erişime Açık
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APA TAN A (2020). Ksantin Oksidaz İnhibitörü Yeni 1,2,3-Triazol Türevlerinin Sentezi, Karakterizasyonu ve Moleküler Doking Çalışmaları. , 644 - 654.
Chicago TAN Ayse Ksantin Oksidaz İnhibitörü Yeni 1,2,3-Triazol Türevlerinin Sentezi, Karakterizasyonu ve Moleküler Doking Çalışmaları. (2020): 644 - 654.
MLA TAN Ayse Ksantin Oksidaz İnhibitörü Yeni 1,2,3-Triazol Türevlerinin Sentezi, Karakterizasyonu ve Moleküler Doking Çalışmaları. , 2020, ss.644 - 654.
AMA TAN A Ksantin Oksidaz İnhibitörü Yeni 1,2,3-Triazol Türevlerinin Sentezi, Karakterizasyonu ve Moleküler Doking Çalışmaları. . 2020; 644 - 654.
Vancouver TAN A Ksantin Oksidaz İnhibitörü Yeni 1,2,3-Triazol Türevlerinin Sentezi, Karakterizasyonu ve Moleküler Doking Çalışmaları. . 2020; 644 - 654.
IEEE TAN A "Ksantin Oksidaz İnhibitörü Yeni 1,2,3-Triazol Türevlerinin Sentezi, Karakterizasyonu ve Moleküler Doking Çalışmaları." , ss.644 - 654, 2020.
ISNAD TAN, Ayse. "Ksantin Oksidaz İnhibitörü Yeni 1,2,3-Triazol Türevlerinin Sentezi, Karakterizasyonu ve Moleküler Doking Çalışmaları". (2020), 644-654.
APA TAN A (2020). Ksantin Oksidaz İnhibitörü Yeni 1,2,3-Triazol Türevlerinin Sentezi, Karakterizasyonu ve Moleküler Doking Çalışmaları. Bitlis Eren Üniversitesi Fen Bilimleri Dergisi, 9(2), 644 - 654.
Chicago TAN Ayse Ksantin Oksidaz İnhibitörü Yeni 1,2,3-Triazol Türevlerinin Sentezi, Karakterizasyonu ve Moleküler Doking Çalışmaları. Bitlis Eren Üniversitesi Fen Bilimleri Dergisi 9, no.2 (2020): 644 - 654.
MLA TAN Ayse Ksantin Oksidaz İnhibitörü Yeni 1,2,3-Triazol Türevlerinin Sentezi, Karakterizasyonu ve Moleküler Doking Çalışmaları. Bitlis Eren Üniversitesi Fen Bilimleri Dergisi, vol.9, no.2, 2020, ss.644 - 654.
AMA TAN A Ksantin Oksidaz İnhibitörü Yeni 1,2,3-Triazol Türevlerinin Sentezi, Karakterizasyonu ve Moleküler Doking Çalışmaları. Bitlis Eren Üniversitesi Fen Bilimleri Dergisi. 2020; 9(2): 644 - 654.
Vancouver TAN A Ksantin Oksidaz İnhibitörü Yeni 1,2,3-Triazol Türevlerinin Sentezi, Karakterizasyonu ve Moleküler Doking Çalışmaları. Bitlis Eren Üniversitesi Fen Bilimleri Dergisi. 2020; 9(2): 644 - 654.
IEEE TAN A "Ksantin Oksidaz İnhibitörü Yeni 1,2,3-Triazol Türevlerinin Sentezi, Karakterizasyonu ve Moleküler Doking Çalışmaları." Bitlis Eren Üniversitesi Fen Bilimleri Dergisi, 9, ss.644 - 654, 2020.
ISNAD TAN, Ayse. "Ksantin Oksidaz İnhibitörü Yeni 1,2,3-Triazol Türevlerinin Sentezi, Karakterizasyonu ve Moleküler Doking Çalışmaları". Bitlis Eren Üniversitesi Fen Bilimleri Dergisi 9/2 (2020), 644-654.