SYNTHESIS AND BIOLOGICAL EVALUATION OF AMINOMETHYL AMIDOMETHN DERIVATIVES OF AN ANTICONVULSANT GAMMA-BUTYROLACTONE/

Authors
AHUNGENA A CANNEY DJ
Citation
A. Ahungena et Dj. Canney, SYNTHESIS AND BIOLOGICAL EVALUATION OF AMINOMETHYL AMIDOMETHN DERIVATIVES OF AN ANTICONVULSANT GAMMA-BUTYROLACTONE/, Medicinal chemistry research, 6(9), 1996, pp. 618-634
Citations number
33
Categorie Soggetti
Chemistry Medicinal
Journal title
Medicinal chemistry research → ACNP
ISSN journal
10542523
Volume
6
Issue
9
Year of publication
1996
Pages
618 - 634
Database
ISI
SICI code
1054-2523(1996)6:9<618:SABEOA>2.0.ZU;2-Y
Abstract
Anticonvulsant alpha-alkyl-substituted gamma-butyrolactones (e.g. 1) a re believed to act at sites on the GABA(A) receptor complex. Novel ami nomethyl and amidomethyl derivatives of alpha-diethyl-gamma-butyrolact one (1), 2 and 3, respectively, were synthesized and evaluated in radi oligand binding assays ([S-35]TBPS; IC50) and for anticonvulsant activ ity (ED(50)). The results suggest that gamma-substitution increases th e toxicity of these lactones and may change their spectrum of anticonv ulsant activity and their mechanism of action.