氟化苯妥英抗惊厥类似物。

Fluorinated phenytoin anticonvulsant analogs.

作者信息

Nelson W L, Kwon Y G, Marshall G L, Hoover J L, Pfeffer G T

出版信息

J Pharm Sci. 1979 Jan;68(1):115-7. doi: 10.1002/jps.2600680141.

Abstract

Six ring-fluorinated phenytoin analogs were synthesized, and their anticonvulsant activity in the maximal electroshock seizure and subcutaneous pentylenetetrazol assays was determined. 5-(4-Fluorophenyl)-5-phenylhydantoin, 5-(3-fluorophenyl)-5-phenylhydantoin, and 5,5-bis(4-fluorophenyl)hydantoin were active in the maximal electroshock seizure assay. The compounds were much less potent than phenytoin but showed an extremely long duration of action.

摘要

合成了六种环氟化苯妥英类似物，并测定了它们在最大电休克惊厥和皮下注射戊四氮试验中的抗惊厥活性。5-(4-氟苯基)-5-苯基乙内酰脲、5-(3-氟苯基)-5-苯基乙内酰脲和5,5-双(4-氟苯基)乙内酰脲在最大电休克惊厥试验中具有活性。这些化合物的效力远低于苯妥英，但作用持续时间极长。