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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

PARHAM TASLIMI, YELİZ DEMİR, HATİCE ESRA DURAN, ÜMİT MUHAMMET KOÇYİĞİT, BURAK TÜZÜN, Osman Nuri Aslan, MUSTAFA CEYLAN, İlhami Gülçin

CUMHURIYET SCIENCE JOURNAL Cilt 42 · Sayı 3 · ss. 553–564 · 01.09.2021
DOI ile aç

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

Atıf için künye

TASLIMI, P., DEMİR, Y., DURAN, H. E., KOÇYİĞİT, 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

BibTeX 
@article{taslimi2021-67678,
  author = {TASLIMI, PARHAM and DEMİR, YELİZ and DURAN, HATİCE ESRA and KOÇYİĞİT, ÜMİT MUHAMMET and TÜZÜN, BURAK and Aslan, Osman Nuri and CEYLAN, MUSTAFA and Gülçin, İlhami},
  title = {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},
  journal = {CUMHURIYET SCIENCE JOURNAL},
  year = {2021},
  volume = {42},
  number = {3},
  pages = {553--564},
  issn = {2587-2680},
  doi = {10.17776/csj.897800},
  url = {https://akademik.atauni.edu.tr/yayinlar/67678-some-old-2-4-aryl-thiazole-2-yl-3a477a-tetrahydro-1h-47-tethanoisoindole-132h}
}