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Synthesis of novel N-benzyl substituted piperidine amides of 1H-indole-5-carboxylic acid as potential inhibitors of cholinesterases
2012
journal article
article
Journal
Acta Poloniae Pharmaceutica. Drug Research
Author
Jakubowska Anna
Kulig Katarzyna
Szałaj Natalia
Malawska Barbara
Volume
69
Number
3
Pages
449-455
ISSN
0001-6837
eISSN
2353-5288
Keywords in English
Alzheimerís disease
acetylcholinesterase inhibitors
butyrylcholinesterase inhibitors
N-benzylpiperidines
1H-indole-5-carboxylic acid derivatives
Access date
2020-07-28
Remarks
Bibliogr. s. 455
Language
English
Journal language
English
Abstract in English
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.
Affiliation
Wydział Farmaceutyczny : Zakład Fizykochemicznej Analizy LekuWydział Farmaceutyczny : Zakład Chemii Organicznej
| 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.source.integrator | false | |
| 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 |
dc.abstract.enpl
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.affiliationpl
Wydział Farmaceutyczny : Zakład Fizykochemicznej Analizy Leku dc.affiliationpl
Wydział Farmaceutyczny : Zakład Chemii Organicznej dc.contributor.authorpl
Jakubowska, Anna - 171114 dc.contributor.authorpl
Kulig, Katarzyna - 130536 dc.contributor.authorpl
Szałaj, Natalia - 140437 dc.contributor.authorpl
Malawska, Barbara - 130819 dc.date.accessionpl
2020-07-28 dc.date.accessioned
2020-07-28T07:42:53Z dc.date.available
2020-07-28T07:42:53Z dc.date.issuedpl
2012 dc.date.openaccess
0 dc.description.accesstime
w momencie opublikowania dc.description.additionalpl
Bibliogr. s. 455 dc.description.numberpl
3 dc.description.physicalpl
449-455 dc.description.publicationpl
0,57 dc.description.version
ostateczna wersja wydawcy dc.description.volumepl
69 dc.identifier.eissnpl
2353-5288 dc.identifier.issnpl
0001-6837 dc.identifier.projectpl
ROD UJ / OP dc.identifier.uri
https://ruj.uj.edu.pl/xmlui/handle/item/242145 dc.identifier.weblinkpl
https://www.ptfarm.pl/wydawnictwa/czasopisma/acta-poloniae-pharmaceutica/110/-/14122 dc.languagepl
eng dc.language.containerpl
eng 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.source.integrator
false dc.subject.enpl
Alzheimerís disease dc.subject.enpl
acetylcholinesterase inhibitors dc.subject.enpl
butyrylcholinesterase inhibitors dc.subject.enpl
N-benzylpiperidines dc.subject.enpl
1H-indole-5-carboxylic acid derivatives dc.subtypepl
Article dc.titlepl
Synthesis of novel N-benzyl substituted piperidine amides of 1H-indole-5-carboxylic acid as potential inhibitors of cholinesterases dc.title.journalpl
Acta Poloniae Pharmaceutica. Drug Research dc.typepl
JournalArticle dspace.entity.type
Publication Affiliations
No affiliation
Jakubowska, Anna
Kulig, Katarzyna
Szałaj, Natalia
Malawska, Barbara
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