Structure-activity studies of fluoroaljyl-substituted γ-butyrolactone and γ-thiobutyrolactone modulators of GABA A receptor function

…, K Xu, KD Holland, SM Rothman, JA Ferrendelli…

Index: Canney, Daniel J.; Lu, Hwang-Fun; McKeon, Ann C.; Yoon, Kong-Woo; Xu, Kun; Holland, Katherine D.; Rothman, Steven M.; Ferrendelli, James A.; Covey, Douglas F. Bioorganic and Medicinal Chemistry, 1998 , vol. 6, # 1 p. 43 - 55

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Citation Number: 28

Abstract

Dihydro-2 (3H)-furanones (γ-butyrolactones) and dihydro-2 (3H)-thiophenones (γ- thiobutyrolactones) containing fluoroalkyl groups at positions C-3, C-4, and C-5 of the heterocyclic rings were prepared. The anticonvulsant/convulsant activities of the compounds were evaluated in mice. Brain concentrations of the compounds were determined and the effects of the compounds on [35S]-tert-butylbicyclophosphorothionate ([35S] TBPS) ...