Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


Preliminary Evaluation of Anticonvulsant Activity of Some Aminoalkanol and Amino Acid Cinnamic Acid Derivatives

Author(s): Agnieszka Gunia, Anna M. Waszkielewicz, Marek Cegla, Henryk Marona.


A series of aminoalkanol and amino acid derivatives of trans-cinnamic acid as well as aminoalkanol derivatives of α-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.

Keywords: Amino acid derivatives, Aminoalkanol derivatives, Anticonvulsant, MES, ScMet, Synthesis, Cinnamic acid derivatives, trans-cinnamic, aminoalkanol, intaperitoneal, pilocarpine, subcutaneous pentetrazole (ScMet), trans-a-phenylcinnamic, Oxytropis pseudoglandulosa, toluene/K2CO3, acylation, polarimeter

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Article Details

Year: 2012
Page: [37 - 43]
Pages: 7
DOI: 10.2174/157018012798192982