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Synthesis and evaluation of anticonvulsant activity of N-(2,5-dimethylphenoxy)- and N-[(2,3,5-trimethylphenoxy)alkyl]aminoalkanols
2015
journal article
article
Journal
Acta Poloniae Pharmaceutica. Drug Research
Author
Waszkielewicz Anna
Gunia-Krzyżak Agnieszka
Cegła Marek
Marona Henryk
Volume
72
Number
1
Pages
89-99
ISSN
0001-6837
eISSN
2353-5288
Keywords in English
anticonvulsant
epilepsy
MES
neurotoxicity
aminoalkanols
synthesis
Access date
2016-10-03
Remarks
Bibliogr. s. 98-99
Language
English
Journal language
English
Abstract in English
A series of new N-(2,5-dimethylphenoxy)- and N-(2,3,5-trimethylphenoxy)alkylaminoalkanols [I-XVII] was synthesized and evaluated for anticonvulsant activity. Pharmacological tests included maximal electroshock (MES) and subcutaneous pentetrazole seizure threshold (scMet) assays as well as neurotoxicity (TOX) evaluation in mice after intraperitoneal (i.p.) administration and/or in rats after oral (p.o.) administration. The most active compound was R-2N-[(2,3,5-trimethylphenoxy)ethyl]aminobutan-1-ol, which exhibited 100% activity in MES at the dose of 30 mg/kg body weight (mice, i.p.) and 75% activity in MES at 30 mg/kg b.w. (rats, p.o.) without neurotoxicity at the active doses.
Affiliation
Wydział Farmaceutyczny : Zakład Chemii BioorganicznejWydział Farmaceutyczny : Zakład Chemii Organicznej
| dc.abstract.en | A series of new N-(2,5-dimethylphenoxy)- and N-(2,3,5-trimethylphenoxy)alkylaminoalkanols [I-XVII] was synthesized and evaluated for anticonvulsant activity. Pharmacological tests included maximal electroshock (MES) and subcutaneous pentetrazole seizure threshold (scMet) assays as well as neurotoxicity (TOX) evaluation in mice after intraperitoneal (i.p.) administration and/or in rats after oral (p.o.) administration. The most active compound was R-2N-[(2,3,5-trimethylphenoxy)ethyl]aminobutan-1-ol, which exhibited 100% activity in MES at the dose of 30 mg/kg body weight (mice, i.p.) and 75% activity in MES at 30 mg/kg b.w. (rats, p.o.) without neurotoxicity at the active doses. | pl |
| dc.affiliation | Wydział Farmaceutyczny : Zakład Chemii Bioorganicznej | pl |
| dc.affiliation | Wydział Farmaceutyczny : Zakład Chemii Organicznej | pl |
| dc.cm.date | 2020-01-07 | |
| dc.cm.id | 70363 | |
| dc.contributor.author | Waszkielewicz, Anna - 242824 | pl |
| dc.contributor.author | Gunia-Krzyżak, Agnieszka - 200092 | pl |
| dc.contributor.author | Cegła, Marek - 128972 | pl |
| dc.contributor.author | Marona, Henryk - 200513 | pl |
| dc.date.accession | 2016-10-03 | pl |
| dc.date.accessioned | 2020-01-17T08:46:13Z | |
| dc.date.available | 2020-01-17T08:46:13Z | |
| dc.date.issued | 2015 | pl |
| dc.date.openaccess | 0 | |
| dc.description.accesstime | w momencie opublikowania | |
| dc.description.additional | Bibliogr. s. 98-99 | pl |
| dc.description.number | 1 | pl |
| dc.description.physical | 89-99 | pl |
| dc.description.points | 15 | pl |
| dc.description.version | ostateczna wersja wydawcy | |
| dc.description.volume | 72 | 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/134836 | |
| dc.identifier.weblink | http://www.ptfarm.pl/pub/File/Acta_Poloniae/2015/1/089.pdf | 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 | anticonvulsant | pl |
| dc.subject.en | epilepsy | pl |
| dc.subject.en | MES | pl |
| dc.subject.en | neurotoxicity | pl |
| dc.subject.en | aminoalkanols | pl |
| dc.subject.en | synthesis | pl |
| dc.subtype | Article | pl |
| dc.title | Synthesis and evaluation of anticonvulsant activity of N-(2,5-dimethylphenoxy)- and N-[(2,3,5-trimethylphenoxy)alkyl]aminoalkanols | pl |
| dc.title.journal | Acta Poloniae Pharmaceutica. Drug Research | pl |
| dc.type | JournalArticle | pl |
| dspace.entity.type | Publication |
dc.abstract.enpl
A series of new N-(2,5-dimethylphenoxy)- and N-(2,3,5-trimethylphenoxy)alkylaminoalkanols [I-XVII] was synthesized and evaluated for anticonvulsant activity. Pharmacological tests included maximal electroshock (MES) and subcutaneous pentetrazole seizure threshold (scMet) assays as well as neurotoxicity (TOX) evaluation in mice after intraperitoneal (i.p.) administration and/or in rats after oral (p.o.) administration. The most active compound was R-2N-[(2,3,5-trimethylphenoxy)ethyl]aminobutan-1-ol, which exhibited 100% activity in MES at the dose of 30 mg/kg body weight (mice, i.p.) and 75% activity in MES at 30 mg/kg b.w. (rats, p.o.) without neurotoxicity at the active doses. dc.affiliationpl
Wydział Farmaceutyczny : Zakład Chemii Bioorganicznej dc.affiliationpl
Wydział Farmaceutyczny : Zakład Chemii Organicznej dc.cm.date
2020-01-07 dc.cm.id
70363 dc.contributor.authorpl
Waszkielewicz, Anna - 242824 dc.contributor.authorpl
Gunia-Krzyżak, Agnieszka - 200092 dc.contributor.authorpl
Cegła, Marek - 128972 dc.contributor.authorpl
Marona, Henryk - 200513 dc.date.accessionpl
2016-10-03 dc.date.accessioned
2020-01-17T08:46:13Z dc.date.available
2020-01-17T08:46:13Z dc.date.issuedpl
2015 dc.date.openaccess
0 dc.description.accesstime
w momencie opublikowania dc.description.additionalpl
Bibliogr. s. 98-99 dc.description.numberpl
1 dc.description.physicalpl
89-99 dc.description.pointspl
15 dc.description.version
ostateczna wersja wydawcy dc.description.volumepl
72 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/134836 dc.identifier.weblinkpl
http://www.ptfarm.pl/pub/File/Acta_Poloniae/2015/1/089.pdf 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.subject.enpl
anticonvulsant dc.subject.enpl
epilepsy dc.subject.enpl
MES dc.subject.enpl
neurotoxicity dc.subject.enpl
aminoalkanols dc.subject.enpl
synthesis dc.subtypepl
Article dc.titlepl
Synthesis and evaluation of anticonvulsant activity of N-(2,5-dimethylphenoxy)- and N-[(2,3,5-trimethylphenoxy)alkyl]aminoalkanols dc.title.journalpl
Acta Poloniae Pharmaceutica. Drug Research dc.typepl
JournalArticle dspace.entity.type
Publication Affiliations
Wydział Farmaceutyczny
Waszkielewicz, Anna
Gunia-Krzyżak, Agnieszka
Cegła, Marek
Marona, Henryk
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