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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    
Yazarlar
Parham Taslımı
Türkiye
Yeliz Demir
Ardahan Üniversitesi, Türkiye
Doç. Dr. Hatice Esra DURAN Doç. Dr. Hatice Esra DURAN
Kafkas Üniversitesi, Türkiye
Ümit Muhammet Koçyiğit
Türkiye
Burak Tüzün
Türkiye
Osman Nuri Aslan
Türkiye
Mustafa Ceylan
Türkiye
İlhami Gülçin
Atatürk Üniversitesi, Türkiye
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.
Anahtar Kelimeler
Makale Türü Özgün Makale
Makale Alt Türü Ulusal alan endekslerinde (TR Dizin, ULAKBİM) yayımlanan tam makale
Dergi Adı Cumhuriyet Science Journal
Dergi ISSN 2587-2680
Dergi Tarandığı Indeksler TR DİZİN
Makale Dili Türkçe
Basım Tarihi 09-2021
Cilt No 42
Sayı 3
Sayfalar 553 / 564
Doi Numarası 10.17776/csj.897800
Makale Linki http://dx.doi.org/10.17776/csj.897800