Journal
LETTERS IN DRUG DESIGN & DISCOVERY
Volume 9, Issue 1, Pages 37-43Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/157018012798192982
Keywords
Amino acid derivatives; Aminoalkanol derivatives; Anticonvulsant; MES; ScMet; Synthesis; Cinnamic acid derivatives
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Funding
- European Regional Development Fund through the Innovative Economy Program
- Jagiellonian University Medical College [K/ZDS/000951, K/DSC/000258]
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A series of aminoalkanol and amino acid derivatives of trans-cinnamic acid as well as aminoalkanol derivatives of alpha-phenylcinnamic acid was synthesized and evaluated for anticonvulsant activity. All compounds were verified in mice after intraperitoneal (i.p.) administration in maximal electroshock (MES) and subcutaneous pentetrazole (ScMet) induced seizures as well as neurotoxicity assessment. Six of them showed protection in MES at 100 mg/kg b.w. and one at 300 mg/kg b.w. For selected derivatives evaluation in ScMet test in rats after per os (p.o.) administration, 6-Hz test in mice and pilocarpine-induced status in rats were performed. The results are quite encouraging and further modification of the structures might lead to discovering new potential anticonvulsants.
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