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, cilt.42, sa.3, ss.553-564, 2021 (TRDizin)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 42 Sayı: 3
- Basım Tarihi: 2021
- Doi Numarası: 10.17776/csj.897800
- Dergi Adı: CUMHURIYET SCIENCE JOURNAL
- Derginin Tarandığı İndeksler: Directory of Open Access Journals, TR DİZİN (ULAKBİM)
- Sayfa Sayıları: ss.553-564
- Açık Arşiv Koleksiyonu: AVESİS Açık Erişim Koleksiyonu
- Atatürk Üniversitesi Adresli: Evet
Özet
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