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Preparation and in vitro testing of bispyridinium inhibitors of cholinesterases - influence of functional groups
 Füri, István ; Opletalová, Veronika (advisor) ; Doležal, Martin (referee)
CHARLES UNIVERSITY IN PRAGUE FACULTY OF PHARMACY IN HRADCI KRÁLOVÉ DEPARTMENT OF PHARMACEUTICAL CHEMISTRY AND DRUG CONTROL Candidate: István Füri Supervisor: Assoc. Prof. RNDr. Veronika Opletalová Ph.D. Diploma Thesis: Preparation and in vitro testing of byspiridine inhibitors of cholinesterases - influence of functional groups In my thesis I was concerned with synthesis and in vitro testing of bispyridinium inhibitors of cholinesterases. Bispyridinium inhibitors were prepared with 8 to 12 carbon chain linkers and naphtyl chain linker with carbamoyl, carbamide or acetyl group in para position in the pyridine ring. In the next step, inhibitory activity of the compounds against AChE and BChE was determined in vitro. The inhibitory activity was measured using modified Ellman's photochemical method. BW-284c51 (for AChE) and ethopropazine (for BChE) were used as standards. Substances with carbamoyl and acetyl functional group showed higher AChE inhibitory activity than compounds with carboxyl functional group. Carboxyl functional group was not suitable for inhibitory activity against BChE, too.
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