N-[(2,6-Dimethylphenoxy)alkyl]aminoalkanols : their physicochemical and anticonvulsant properties
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dc.type
JournalArticle
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dc.description.physical
4197-4217
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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.
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dc.subject.en
6 Hz
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dc.subject.en
anticonvulsant activity
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dc.subject.en
ames test
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dc.subject.en
crystal structure
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dc.subject.en
aminoalkanols
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dc.subject.en
DSC
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dc.subject.en
mutagenicity
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dc.subject.en
MES
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dc.subject.en
rotarod
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dc.subject.en
TG
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dc.subject.en
seizures
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dc.subject.en
TOX
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dc.description.volume
23
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dc.description.number
15
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dc.description.points
30
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dc.identifier.doi
10.1016/j.bmc.2015.06.045
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dc.identifier.eissn
1464-3391
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dc.title.journal
Bioorganic & Medicinal Chemistry
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dc.language.container
eng
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dc.affiliation
Wydział Farmaceutyczny : Zakład Chemii Bioorganicznej
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dc.affiliation
Wydział Farmaceutyczny : Zakład Biochemii Farmaceutycznej
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dc.affiliation
Wydział Chemii : Zakład Krystalochemii i Krystalofizyki
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dc.affiliation
Wydział Farmaceutyczny : Zakład Chemii Organicznej