PARTIAL STRUCTURES OF THE FUNGAL TOXIN AFLATREM, METHYL-SUBSTITUTED 6,8-DIOXABICYCLO[3.2.1]OCTAN-2-ONES HAVE ANTICONVULSANT ACTIVITY

Authors
TINAOWOOLDRIDGE LV HSIANG BCH LATIFI TN FERRENDELLI JA COVEY DF
Citation
Lv. Tinaowooldridge et al., PARTIAL STRUCTURES OF THE FUNGAL TOXIN AFLATREM, METHYL-SUBSTITUTED 6,8-DIOXABICYCLO[3.2.1]OCTAN-2-ONES HAVE ANTICONVULSANT ACTIVITY, Bioorganic & medicinal chemistry letters, 5(3), 1995, pp. 265-270
Citations number
16
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
3
Year of publication
1995
Pages
265 - 270
Database
ISI
SICI code
0960-894X(1995)5:3<265:PSOTFT>2.0.ZU;2-L
Abstract
4,7,7-Trimethyl-6,8-dioxabicyclo[3.2.1]octan-2-one was found to be an effective anticonvulsant (ED(50) = 131 mg/kg) against pentylenetetrazo le-induced seizures in mice. Enantioselectively was observed in the ac tions of the (+)- and (-)-enantiomers as anticonvulsants and as displa cers of [S-35]-TPBS, a ligand for the picrotoxin site on GABA(A) recep tors. The (-)- enantiomer was slightly more potent in both biological assays.