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    Erratum: Evaluation of benzaldehyde derivatives as being bovine kidney aldose reductase inhibitors
    (2023) Sengül, Bülent
    Aldose reductase (AR) catalyzes the production of sorbitol from glucose in the polyol pathway, and it is a critical enzyme that causes an aberrant aggregation of sorbitol in insulin- independent tissues, create some problems including retinopathy, neuropathy, and nephropathy. AR inhibition has been shown to be a viable approach for reducing these side effects. The current study aimed to introduce new AR inhibitors to the literature. For this purpose, benzaldehydes were examined as being AR inhibitors. Firstly, the homogenate was prepared from the bovine kidney, then inhibition studies were carried out. It was found that all derivatives inhibited AR. The inhibitory potency of 4- Phenyl benzaldehyde (3) and 2- Bromobenzaldehyde (6), having IC50 values as 0.23 and 1.37 ?M, respectively, was determined higher than standard inhibitor sorbinil. After in vitro inhibition studies, estimated binding energies and binding modes of derivatives with enzyme were predicted by molecular docking. Compound 3 exhibited a maximum docking score of -8,61 kcal/mol. In conclusion, these compounds especially compound 3 may be guiding agents that can be used to synthesize new drug candidate molecules to treat or prevent diabetic complications.
  • Küçük Resim Yok
    Öğe
    Evaluation of benzaldehyde derivatives as being bovine kidney aldose reductase inhibitors
    (2023) Sengül, Bülent
    Aldose reductase (AR) catalyzes the production of sorbitol from glucose in the polyol pathway, and it is a critical enzyme that causes an aberrant aggregation of sorbitol in insulin- independent tissues, create some problems including retinopathy, neuropathy, and nephropathy. AR inhibition has been shown to be a viable approach for reducing these side effects. The current study aimed to introduce new AR inhibitors to the literature. For this purpose, benzaldehydes were examined as being AR inhibitors. Firstly, the homogenate was prepared from the bovine kidney, then inhibition studies were carried out. It was found that all derivatives inhibited AR. The inhibitory potency of 4- Phenyl benzaldehyde (3) and 2- Bromobenzaldehyde (6), having IC50 values as 0.23 and 1.37 ?M, respectively, was determined higher than standard inhibitor sorbinil. After in vitro inhibition studies, estimated binding energies and binding modes of derivatives with enzyme were predicted by molecular docking. Compound 3 exhibited a maximum docking score of -8,61 kcal/mol. In conclusion, these compounds especially compound 3 may be guiding agents that can be used to synthesize new drug candidate molecules to treat or prevent diabetic complications.