Autors: Valentin R. Karabeliov., Magdalena S. Kondeva-Burdina., Nikolay G. Vassilev., Yovkova, E. K., Violina T. Angelova.
Title: Neuroprotective evaluation of novel substituted 1,3,4-oxadiazole and aroylhydrazone derivatives
Keywords: ADME; Hydrazones; Neurodegenerative disorder; Neuroprotectio

Abstract: The paper reports on the facile and convenient synthesis of a series of novel 2,5-substituted 1,3,4-oxadiazoles 3a-f and that of aroylhydrazone-based molecular hybrids 5a-g from readily available starting materials. The structure of the compounds was confirmed by IR, 1H NMR, 13C NMR and HRESI-MS spectral data. The toxicological potential of the compounds was evaluated by monitoring the synaptosomal viability and the levels of reduced glutathione in rat brain synaptosomes, isolated by Percoll gradient. The neuroprotective effects were assessed in vitro in a model of 6-hydroxydopamine-induced neurotoxicity. Two of the compounds from the novel oxadiazoles 3a and 3d did not have any toxicity. In a model of 6-OHDA-induced oxidative stress 5a-g revealed statistically significant neuroprotective effect. Some of the compounds may have neuroprotective effects due to possible stabilization of the synaptosomal membrane. All the compounds display a good predicted ADME profile.

References

    Issue

    Bioorganic & Medicinal Chemistry Letters, vol. 59, issue 1, pp. 128516, 2022, Netherlands, Elsevier, ISSN 0960-894X; https://doi.org/10.1016/j.bmcl.2021.128516

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    Вид: статия в списание, публикация в издание с импакт фактор, публикация в реферирано издание, индексирана в Scopus