TY - JOUR
T1 - Partial structures of the fungal toxin aflatrem, methyl-substituted 6,8-dioxabicyclo[3.2.1]octan-2-ones have anticonvulsant activity
AU - Tinao-Wooldridge, Luzviminda V.
AU - Hsiang, Bonnie C.H.
AU - Latifi, Tammy N.
AU - Ferrendelli, James A.
AU - Covey, Douglas F.
N1 - Funding Information:
Barry Sharpless for assistance in assigning the absolute configuration of the 1,2-dihydroxylation products. This work was supported by National Institutes of Health grant NS14834. Assistance was also provided by the Washington University High Resolution NMR Facility supported in part by National Institutes of Health grant 1 S10 RR00204 and a gift from the Monsanto Co.
PY - 1995/2/2
Y1 - 1995/2/2
N2 - 4,7,7-Trimethyl-6,8-dioxabicyclo[3.2.1]octan-2-one was found to be an effective anticonvulsant (ED50 = 131 mg/kg) against pentylenetetrazole-induced seizures in mice. Enantioselectively was observed in the actions of the (+)- and (-)-enantiomers as anticonvulsants and as displacers of [35S]-TPBS, a ligand for the picrotoxin site on GABAA receptors. The (-)-enantiomer was slightly more potent in both biological assays.
AB - 4,7,7-Trimethyl-6,8-dioxabicyclo[3.2.1]octan-2-one was found to be an effective anticonvulsant (ED50 = 131 mg/kg) against pentylenetetrazole-induced seizures in mice. Enantioselectively was observed in the actions of the (+)- and (-)-enantiomers as anticonvulsants and as displacers of [35S]-TPBS, a ligand for the picrotoxin site on GABAA receptors. The (-)-enantiomer was slightly more potent in both biological assays.
UR - http://www.scopus.com/inward/record.url?scp=0028869935&partnerID=8YFLogxK
U2 - 10.1016/0960-894X(95)00021-K
DO - 10.1016/0960-894X(95)00021-K
M3 - Article
AN - SCOPUS:0028869935
SN - 0960-894X
VL - 5
SP - 265
EP - 270
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 3
ER -