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- Title
Synthesis and Anticonvulsant Activity of New Calix[4]Arene Derivatives Containing Gamma-Aminobutyric Acid Moieties.
- Authors
Nesterkina, M.; Alekseeva, E.; Kravchenko, I.
- Abstract
A series of novel mono- and disubstituted p- tert-butylcalix[4]arene derivatives functionalized with gamma-aminobutyric acid (GABA) and its methyl ester were synthesized and screened in vivo for anticonvulsant activity by determining the minimum effective doses of pentylenetetrazole inducing clonic-tonic convulsions and tonic extension. Calixarene derivative X with one acetic acid and one GABA ester on the lower rim of the macrocyclic scaffold was characterized as possessing prolonged anticonvulsant activity. A relationship between the pharmacological effect and the number of amino-acid residues was found. Disubstituted calixarenes IV and IX demonstrated higher anticonvulsant activity 24 h after administration than the monosubstituted analogs.
- Subjects
CALIXARENES synthesis; ANTICONVULSANTS; CALIXARENE derivatives; GABA; MOIETIES (Chemistry); DRUG dosage
- Publication
Pharmaceutical Chemistry Journal, 2016, Vol 49, Issue 12, p825
- ISSN
0091-150X
- Publication type
Article
- DOI
10.1007/s11094-016-1380-7