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Title: Synthesis and properties of heterodimeric structures as potential inhibitors of cholinesterases


The dissertation presents current trends in searching for inhibitors of the cholinesterases including multi-target directed ligands as potential drugs for AD. Research concerned synthesis of heterodimeric compounds with acetylcholinesterease and/or butyrylcholinesterase inhibiton properties and inhibition of β-amyloid aggregation.Seven series of heterodimeric compounds were obtained with indole, phtalimide or tetrahydoisochinoline moiety connected byalkyl or p-ksylene linker with an amine. Chromatographic parameter of lipophilicity RM0 for each compound were determined by using reverse phase chromatography and also parameter log P was determined using calculation programs.Obtained compounds were tested for ability to inhibit cholinesterases in spectrophotometric assay Ellman test. All compounds inhibit AChE and 17 compounds were active against BuChE. The most active compound is 2-(7-(pirolidinoheptylo)isoindolino-1,3-dion hydrochloride 31a (IC50 = 0,27 µM) and is selective against AChE.Two series of compounds were tested against inhibiting β-amyloid aggregation.Compound 13a 2-(7-diethylo-aminoheptylo)isoindolino-1,3-dion hydrochloride has the best procent of inhibiting β-amyloid (39,4% in 80 µM), moreover has good activity an selectivity against AChe (IC50 = 0,43 µM). The results of molecular modeling studies indicate that the ability to interact in both the catalytic and perip ; heral binding site of the enzyme, which confirms the dual activity of the compound 13a.

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2 - studia doktoranckie

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Wydział Farmaceutyczny


Malawska, Barbara

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pol; eng

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tylko w bibliotece

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Mar 15, 2023

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May 30, 2014

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ZB-120653 Mar 15, 2023


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