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Antioxidant Properties, Neuroprotective Effects and in Vitro Safety Evaluation of New Pyrrole Derivatives

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Pharmaceutical Chemistry Journal Aims and scope

The paper is focused on safety evaluation, antioxidant activity and neuroprotective properties determination of newly synthesized substituted N-pyrrolyl hydrazide hydrazones on two neuronal in vitro models: human neuronal cells SH-SY5Y and isolated rat brain synaptosomes. Preliminary toxicological data indicated low or no in vitro toxicity for all evaluated substances, where compounds 9a and 9d were extracted as safest and most promising structures with lowest neurotoxicity. Performed neuroprotective evaluations showed statistically significant neuroprotective effects on two applied models of induced oxidative stress, with most pronounced effect observed for 9a being comparable with that of melatonin. Statistically significant inhibitory activity on human recombinant MAO-B enzyme, close to that of selegiline and better than that melatonin, was only found for compound 9a.

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CONFLICT OF INTEREST

The authors declare that they have no conflicts of interest.

Funding

This work was supported by the Bulgarian Ministry of Education and Science under the National Program for Research “Young Scientists and Postdoctoral Students.”

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Authors and Affiliations

  1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Medical University – Sofia, 2 Dunav str, 1000, Sofia, Bulgaria

    Diana Tzankova, Maya Georgieva & Lily Peikova

  2. Department of Organic Synthesis and Fuels, University of Chemical Technology and Metallurgy, 8 Kl. Ohridski, 1756, Sofia, Bulgaria

    Stanislava Vladimirova

  3. Department of Pharmacology, Pharmacotherapy and Toxicology, Faculty of Pharmacy - Medical University – Sofia, 2 Dunav str, 1000, Sofia, Bulgaria

    Denitsa Aluani, Magdalena Kondeva-Burdina & Virginia Tzankova

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  1. Diana Tzankova
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  2. Denitsa Aluani
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  4. Maya Georgieva
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  5. Stanislava Vladimirova
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  7. Virginia Tzankova
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Correspondence to Diana Tzankova.

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Tzankova, D., Aluani, D., Kondeva-Burdina, M. et al. Antioxidant Properties, Neuroprotective Effects and in Vitro Safety Evaluation of New Pyrrole Derivatives. Pharm Chem J 55, 1310–1319 (2022). https://doi.org/10.1007/s11094-022-02577-3

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  • DOI: https://doi.org/10.1007/s11094-022-02577-3

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