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Title: Novel cholinesterases inhibitors with carbamoyloxyphenyl and N-benzylpiperidine moieties
Abstract:
The aim of this study was research in the field of new cholinesterases inhibitors. In the introductory part of the dissertation history, epidemiology and etiology of Alzheimer’s disease (AD) were briefly presented. Current trends in research of effective drugs for AD with an emphasis put on the acetyl- and butyrylcholiesterase (AChE, BuChE) inhibitors are discussed in detail. Several series of the new compounds bearing carbamoyloxyphenyl and Nbenzylpiperidine moieties that can be found in antialzheimer’s drug such as rivastigmine or donepezil have been obtained. The activity of the obtained products was tested in vitro with the spectrometric method of Ellman. The most interesting series of inhibitors was hybrid molecules bearing two moieties: 1-benzylpiperidino-4-amino group and heterocyclic indol ring or izoindolino-1,3- dion linked by alkyl chains of different lengths. Izoindolino-1,3-dion derivative with an octyl linker characterized by a balanced mode of action against AChE and BuChE was selected for further investigation. Molecular modeling studies revealed possible interactions between the investigated molecules and both the catalytic and the peripheral active sites of acetylcholinesterase. For the selected compounds the lipophilicity parameters were determined by the experimental chromatographical (RP-TLC, RP-HPLC) and computational methods. Such dual bindig site ligand ; s in the N-benzylpiperidine series constitute a first generation of potent inhibitors which can be used for further development.
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Last modified:
Jul 21, 2022
In our library since:
Nov 21, 2012
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14
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All available object's versions:
http://dl.cm-uj.krakow.pl:8080/publication/1048
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| Edition name | Date |
|---|---|
| ZB-108270 | Jul 21, 2022 |
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