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Synthesis of novel N-benzyl substituted piperidine amides of 1H-indole-5-carboxylic acid as potential inhibitors of cholinesterases
Alzheimerís disease
acetylcholinesterase inhibitors
butyrylcholinesterase inhibitors
N-benzylpiperidines
1H-indole-5-carboxylic acid derivatives
A series of novel N-benzyl substituted amides of 1H-indole-5-carboxylic acid were synthesized and evaluated for their ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The target compounds (6bñ6e) displayed moderate potency to inhibit BuChE. One of the compounds tested, i.e., 1- benzylpiperidine amide of 1H-indole-5-carboxylic acid (6a) was a weak, non-selective inhibitor for both enzymes. The highest inhibitory activity towards BuChE (30.06% [10 μM]) was determined for compound (6c) which is 1-(3-chloro)benzylpiperidine amide of 1H-indole-5-carboxylic acid.
| dc.abstract.en | A series of novel N-benzyl substituted amides of 1H-indole-5-carboxylic acid were synthesized and evaluated for their ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The target compounds (6bñ6e) displayed moderate potency to inhibit BuChE. One of the compounds tested, i.e., 1- benzylpiperidine amide of 1H-indole-5-carboxylic acid (6a) was a weak, non-selective inhibitor for both enzymes. The highest inhibitory activity towards BuChE (30.06% [10 μM]) was determined for compound (6c) which is 1-(3-chloro)benzylpiperidine amide of 1H-indole-5-carboxylic acid. | pl |
| dc.affiliation | Wydział Farmaceutyczny : Zakład Fizykochemicznej Analizy Leku | pl |
| dc.affiliation | Wydział Farmaceutyczny : Zakład Chemii Organicznej | pl |
| dc.contributor.author | Jakubowska, Anna - 171114 | pl |
| dc.contributor.author | Kulig, Katarzyna - 130536 | pl |
| dc.contributor.author | Szałaj, Natalia - 140437 | pl |
| dc.contributor.author | Malawska, Barbara - 130819 | pl |
| dc.date.accession | 2020-07-28 | pl |
| dc.date.accessioned | 2020-07-28T07:42:53Z | |
| dc.date.available | 2020-07-28T07:42:53Z | |
| dc.date.issued | 2012 | pl |
| dc.date.openaccess | 0 | |
| dc.description.accesstime | w momencie opublikowania | |
| dc.description.additional | Bibliogr. s. 455 | pl |
| dc.description.number | 3 | pl |
| dc.description.physical | 449-455 | pl |
| dc.description.publication | 0,57 | pl |
| dc.description.version | ostateczna wersja wydawcy | |
| dc.description.volume | 69 | pl |
| dc.identifier.eissn | 2353-5288 | pl |
| dc.identifier.issn | 0001-6837 | pl |
| dc.identifier.project | ROD UJ / OP | pl |
| dc.identifier.uri | https://ruj.uj.edu.pl/xmlui/handle/item/242145 | |
| dc.identifier.weblink | https://www.ptfarm.pl/wydawnictwa/czasopisma/acta-poloniae-pharmaceutica/110/-/14122 | pl |
| dc.language | eng | pl |
| dc.language.container | eng | pl |
| dc.rights | Udzielam licencji. Uznanie autorstwa - Użycie niekomercyjne 4.0 Międzynarodowa | * |
| dc.rights.licence | CC-BY-NC | |
| dc.rights.uri | http://creativecommons.org/licenses/by-nc/4.0/legalcode.pl | * |
| dc.share.type | otwarte czasopismo | |
| dc.subject.en | Alzheimerís disease | pl |
| dc.subject.en | acetylcholinesterase inhibitors | pl |
| dc.subject.en | butyrylcholinesterase inhibitors | pl |
| dc.subject.en | N-benzylpiperidines | pl |
| dc.subject.en | 1H-indole-5-carboxylic acid derivatives | pl |
| dc.subtype | Article | pl |
| dc.title | Synthesis of novel N-benzyl substituted piperidine amides of 1H-indole-5-carboxylic acid as potential inhibitors of cholinesterases | pl |
| dc.title.journal | Acta Poloniae Pharmaceutica. Drug Research | pl |
| dc.type | JournalArticle | pl |
| dspace.entity.type | Publication |
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