Vývoj insekticidů inhibující acetylcholinesterasu

Mányová, Brigita

Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Brigita Mányová Supervisor: PharmDr. Marie Vopršalová, CSc. Supervisor-specialist: PharmDr. Vendula Hepnarová, Ph.D. Title of diploma thesis: Development of insecticides inhibiting acetylcholineseterase Pest insects cause problems and damage all over the world. They are vectors of serious diseases such as malaria, dengue fever, yellow fever, Zika virus disease and chikungunya disease. They cause huge damage to agricultural crops and are annoying to everyday life in living spaces. The aim of this diploma thesis was in vitro testing of selected compounds from the group of bis-isoquinoline and bispyridinium acetylcholinesterase inhibitors as potential insecticides. Another goal was also to create relationships between structure and effect. The ability of these compounds to inhibit both human (hAChE) and fly acetylcholinesterase (MdAChE) was evaluated. The modified Ellman spectrophotometric method was used. The half inhibitory concentration (IC50) values were obtained for both enzymes and the selectivity indexes (SI) were then calculated. Compounds having IC50s in micromolar or nanomolar range and exhibiting selectivity for MdAChE were most desirable. During the testing of these inhibitors, three...

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