Some old 2-(4-(Aryl)- thiazole-2-yl)-3a,4,7,7a-tetrahydro-1H-4,7-tethanoisoindole-1,3(2H)-dione derivatives: Synthesis, inhibition effects and molecular docking studies on Aldose reductase and α-Glycosidase

Parham Taslımı; Yeliz Demir; Hatice Esra Duran; Ümit Muhammet Koçyiğit; Burak Tüzün; Osman Nuri Aslan; Mustafa Ceylan; İlhami Gülçin

doi:10.17776/csj.897800

TR EN

Öz

Basit kromatik teknikler kullanılarak Aldoz redüktaz AR, koyun karaciğerinden elde edildi. Ek olarak, Saccharomyces cerevisiae'den elde edilen a-glikosidaz enzim olarak kullanıldı. Bileşikler ve enzimler arasındaki etkileşimler belirlendi. Moleküllerin biyolojik aktivite değerlerini enzimlerle karşılaştırmak için kullanılan moleküler yerleştirme yöntemi. Bu çalışmada, sentetik izoindol ikame tiyazol türevlerinin (3a-f) aldoz redüktaz ve α-glikozidaz enzimleri üzerindeki inhibisyon etkisi incelenmiştir. Tiyazol serisinde, bileşik 3b (Ki: 9.70 ± 4.72 M), AR'ye karşı maksimum bir inhibitör etki gösterirken, bileşik 3f (Ki: 44.40 ± 17.18 M), AR'ye karşı en düşük bir inhibitör etki gösterdi. Α-glikozidaza karşı Ki değerleri 24.54 ± 6.92–44.25 ± 10.34 M aralığında olan güçlü inhibisyon profilleri araştırıldı. Teorik sonuçlar deneysel sonuçlarla uyumlu bulundu. Antidiyabetik maddeler olarak hareket eden bu bileşikler, AR ve a-glikosidaz enzimlerinin seçici inhibitörü olma potansiyeline sahiptir. Çalışılan moleküllerin Aldoz redüktaz ve α-glikosidaz enzimlerine karşı biyolojik aktiviteleri moleküler yerleştirme yöntemi ile karşılaştırılacaktır. Moleküllerin ADME analizi (Absorpsiyon, dağılım, metabolizma, atılım ve toksisite) yapılacaktır.

Anahtar Kelimeler

Supporting Institution

Sivas Cumhuriyet University

Project Number

RGD-020

Thanks

This work is supported by the Scientific Research Project Fund of Sivas Cumhuriyet University under the project number RGD-020. This research was made possible by TUBITAK ULAKBIM, High Performance and Grid Computing Center (TR-Grid e-Infrastructure).

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Details

Primary Language

English

Subjects

Structural Biology

Journal Section

Research Article

Authors

Parham Taslımı
0000-0002-3171-0633
Türkiye

Yeliz Demir
Türkiye

Hatice Esra Duran
Türkiye

Ümit Muhammet Koçyiğit
Türkiye

Burak Tüzün ^*
0000-0002-0420-2043
Türkiye

Osman Nuri Aslan
0000-0002-1330-6194
Türkiye

Mustafa Ceylan
Türkiye

İlhami Gülçin
0000-0001-5993-1668
Türkiye

Publication Date

September 24, 2021

Submission Date

March 16, 2021

Acceptance Date

September 20, 2021

Published in Issue

Year 1970 Volume: 42 Number: 3

DOI

https://doi.org/10.17776/csj.897800

IZ

https://izlik.org/JA57NL55JK

Cite

RIS / Bibtex

APA

Taslımı, P., Demir, Y., Duran, H. E., Koçyiğit, Ü. M., Tüzün, B., Aslan, O. N., Ceylan, M., & Gülçin, İ. (2021). Some old 2-(4-(Aryl)- thiazole-2-yl)-3a,4,7,7a-tetrahydro-1H-4,7-tethanoisoindole-1,3(2H)-dione derivatives: Synthesis, inhibition effects and molecular docking studies on Aldose reductase and α-Glycosidase. Cumhuriyet Science Journal, 42(3), 553-564. https://doi.org/10.17776/csj.897800