Romanian Society of Pharmaceutical Sciences
 

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EVALUATION OF THE IN VITRO NEUROTOXIC AND NEUROPROTECTIVE EFFECTS AT CELLULAR AND SUBCELLULAR LEVELS OF NEWLY SYNTHESIZED N-PYRROLYL HYDRAZONES

DIANA TZANKOVA 1*, STANISLAVA VLADIMIROVA 2, DENITSA STEFANOVA 3, LILY
PEIKOVA 1, MAGDALENA KONDEVA-BURDINA 3, MAYA GEORGIEVA 1

1Department of Pharmaceutical Chemistry, Faculty of Pharmacy – Medical University – Sofia, 2 Dunav Street, 1000 Sofia, Bulgaria
2Department of Organic Synthesis and Fuels, University of Chemical Technology and Metallurgy, 8 Kl. Ohridski, 1756 Sofia, Bulgaria
3Department of Pharmacology, Pharmacotherapy and Toxicology, Faculty of Pharmacy – Medical University – Sofia, 2 Dunav
Street, 1000 Sofia, Bulgaria

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The study presents the safety, antioxidant activity and neuroprotective effects of a series of newly synthesized N-pyrrolyl hydrazide-hydrazones (5, 5a-g) in two in vitro models: human neuronal cells SH-SY5Y and isolated rat brain synaptosomes. The performed in vitro toxicological evaluation in neuronal SH-SY5Y cell line models determined the lowest cytotoxicity and best safety profile for compound 5a, followed by 5d on both evaluated parameters. The protective effect of the newly synthesized hydrazone 5a was found to be comparable to melatonin used as a standard. The obtained results indicate that the presence of pyrrole ring, containing multiple phenyl nuclei and hydrazide-hydrazone group in the side chain, leads to increase in the antioxidant effect.