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

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

doi:10.17776/csj.897800

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 (8)

Parham Taslımı Bartın Üniversitesi, Türkiye

Yeliz Demir Ardahan Üniversitesi, Türkiye

Doç. Dr. Hatice Esra DURAN Kafkas Üniversitesi, Türkiye

Ümit Muhammet Koçyiğit Türkiye

Burak Tüzün Sivas Cumhuriyet Üniversitesi, Türkiye

Osman Nuri Aslan Tokat Gaziosmanpaşa Üniversitesi, Türkiye

Mustafa Ceylan Tokat Gaziosmanpaşa Üniversitesi, Türkiye

İlhami Gülçin Atatürk Üniversitesi, Türkiye

Makale Türü	Özgün Makale (Ulusal alan endekslerinde (TR Dizin, ULAKBİM) yayınlanan tam makale)
Dergi Adı	Cumhuriyet Science Journal
Dergi ISSN	2587-2680
Dergi Tarandığı Indeksler	TR DİZİN
Makale Dili	İngilizce	Basım Tarihi	09-2021
Cilt / Sayı / Sayfa	42 / 3 / 553–564	DOI	10.17776/csj.897800
Makale Linki	http://dx.doi.org/10.17776/csj.897800

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.

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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

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

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