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N-[(2,6-Dimethylphenoxy)alkyl]aminoalkanols : their physicochemical and anticonvulsant properties

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N-[(2,6-Dimethylphenoxy)alkyl]aminoalkanols : their physicochemical and anticonvulsant properties

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dc.contributor.author Waszkielewicz, Anna [SAP20012444] pl
dc.contributor.author Cegła, Marek [SAP20001397] pl
dc.contributor.author Żesławska, Ewa pl
dc.contributor.author Nitek, Wojciech [SAP12014773] pl
dc.contributor.author Słoczyńska, Karolina [SAP20011454] pl
dc.contributor.author Marona, Henryk [SAP20000903] pl
dc.date.accessioned 2015-12-09T10:11:42Z
dc.date.available 2015-12-09T10:11:42Z
dc.date.issued 2015 pl
dc.identifier.issn 0968-0896 pl
dc.identifier.uri http://ruj.uj.edu.pl/xmlui/handle/item/17919
dc.language eng pl
dc.title N-[(2,6-Dimethylphenoxy)alkyl]aminoalkanols : their physicochemical and anticonvulsant properties pl
dc.type JournalArticle pl
dc.description.physical 4197-4217 pl
dc.abstract.en Twenty four new N-[(dimethylphenoxy)alkyl]aminoalkanols have been synthesized and evaluated for anticonvulsant activity in a series of in vivo tests: the maximum electroshock (MES), 6 Hz, and subcutaneous metrazole (ScMet). The compounds were also evaluated for possible neurotoxicity in the rotarod test. The majority of the achieved compounds exhibit quantified anticonvulsant activity. The most active compound 4: R-(−)-2N-[(2,6-dimethylphenoxy)ethyl]aminopropan-1-ol is active in MES with ED50 = 5.34 (male mice, ip), 22.28 (female mice, ip), 51.19 (male mice, po), 7.43 (rats, ip), and 28.60 (rats, po). Thermal analysis proved that its hydrochloride (4a) can exist in polymorphic forms. The compound binds to σ, 5-HT1A, and α2 receptors as well as 5-HT transporter and it does not exhibit mutagenic properties. pl
dc.subject.en 6 Hz pl
dc.subject.en anticonvulsant activity pl
dc.subject.en ames test pl
dc.subject.en crystal structure pl
dc.subject.en aminoalkanols pl
dc.subject.en DSC pl
dc.subject.en mutagenicity pl
dc.subject.en MES pl
dc.subject.en rotarod pl
dc.subject.en TG pl
dc.subject.en seizures pl
dc.subject.en TOX pl
dc.description.volume 23 pl
dc.description.number 15 pl
dc.description.points 30 pl
dc.identifier.doi 10.1016/j.bmc.2015.06.045 pl
dc.identifier.eissn 1464-3391 pl
dc.title.journal Bioorganic & Medicinal Chemistry pl
dc.language.container eng pl
dc.affiliation Wydział Farmaceutyczny : Zakład Chemii Bioorganicznej pl
dc.affiliation Wydział Farmaceutyczny : Zakład Biochemii Farmaceutycznej pl
dc.affiliation Wydział Chemii : Zakład Krystalochemii i Krystalofizyki pl
dc.affiliation Wydział Farmaceutyczny : Zakład Chemii Organicznej pl
dc.subtype Article pl
dc.rights.original bez licencji pl
dc.cm.id 73596
.pointsMNiSW [2015 A]: 30


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