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30th Annual European Pharma Congress

Berlin, Germany

 Valentin R. Karabelyov

Valentin R. Karabelyov

Department Pharmacology, Pharmacotherapy and Toxicology”, Faculty of Pharmacy, Medical University-Sofia, Bulgaria

Title: Design and in vitro evaluation of possible MAOB activity of 1,3,4-oxadiazole derivatives and melatonin analogues

Biography

Biography: Valentin R. Karabelyov

Abstract

 

Based on our previous investigation, two different classes of compounds - 1,3,4-oxadiazole derivatives (3a-3e) and melatonin analogues (5a-5e) were synthesized and evaluated for their neuroprotective effect. The aim of our study was to investigate activity in vitro of novel compounds on hMAOB enzyme. Monoaminoxidase activity assay of recombinant human MAOB was performed using a fluorometric method by Amplex UltraRed reagent [1] with small modifications, where Tyramine hydrochloride was used as a substrate. Of the substances tested, 3a and 3d exhibit a statistically significant inhibitory effect on MAOB, commensurate with that of selegiline. The results suggest that some of the oxadiazoles may show promising results in other in vitro models resembling Parkinson's disease.