The synthesis of new oxindoles as analogs of natural product 3,3 `-bis(indolyl)oxindole and in vitro evaluation of the enzyme activity of G6PD and 6PGD
Tarih
2018Yazar
Bayindir, Sinan and Ayna, Adnan and Temel, Yusuf and Ciftci, Mehmet
Üst veri
Tüm öğe kaydını gösterÖzet
Natural and synthetic derivatives that contain an indole core are being
used in medical treatments and technological processes. Therefore, the
development of new synthetic methods for the synthesis of indole
derivatives is very popular. In this study, new oxindoles with reaction
of 4,7-dihydro-1H-indole (2) and isatin (4) were synthesized as analogs
of natural product 3,3'-bis(indolyl)oxindole. The biological properties
of the compounds obtained during this study were also studied, showing
that compounds 5, 7, and 12 inhibited the activity of G6PD with an IC50
of 99 mu M, 231 mu M, and 304 mu M respectively. The activity of rat
erythrocyte 6PGD was increased in the presence of 5 and 7 and was
inhibited in the presence of 12. As indole derivative 5 was an activator
of 6PGD and inhibitor of G6PD, it was selected for docking studies to
understand the mechanism of activation and inhibition.
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