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

Yıl 2021, Cilt: 42 Sayı: 3, 553 - 564, 24.09.2021

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

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

Cited By: 3

Öz

Utilizing the simple chromatic techniques, Aldose reductase (AR) was derived from sheep liver. In addition, α-glycosidase from Saccharomyces cerevisiae was used as the enzyme. It was determined the interactions between compounds and the enzymes. Molecular docking method used to compare biological activity values of molecules against enzymes.
In the current study, the inhibition effect of synthetic isoindol-substitute thiazole derivatives (3a-f) on AR, and α-glycosidase enzymes was studied. In the thiazole series, compound 3b (Ki: 9.70±4.72 M) showed a maximum inhibitory impact towards AR while compound 3f (Ki: 44.40±17.18 M) showed a lowest inhibitory impact towards AR. It was investigated potent inhibition profiles with Ki values in the range of 24.54±6.92–44.25±10.34 M against α-glycosidase. Theoretical results were found consistent with experimental results.
Acting as antidiabetic agents, these compounds have the potential to be the selective inhibitor of α-glycosidase and AR enzymes. The biological activities of the studied molecules against AR and α-glycosidase enzymes will be compared with molecular docking method. ADME analysis of the molecules will be done.

Anahtar Kelimeler

Asymmetric synthesis, Enzyme inhibition, Aldose reductase, α-Glycosidase, Molecular docking

Destekleyen Kurum

Sivas Cumhuriyet University

Proje Numarası

RGD-020

Teşekkür

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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