Kelley J L, Koble C S, Davis R G, McLean E W, Soroko F E, Cooper B R
Division of Organic Chemistry, Burroughs Wellcome Co., Research Triangle Park, North Carolina 27709, USA.
J Med Chem. 1995 Sep 29;38(20):4131-4. doi: 10.1021/jm00020a030.
A series of (fluorobenzyl)triazolo[4,5-c]pyridines was synthesized and tested for activity against maximal electroshock-induced seizures in rodents. The most promising compound, 14 (BW 534U87), which is a carbon-nitrogen isoster of a purine anticonvulsant, has a profile in rodents that suggests 14 will be free of emesis and useful in the treatment of seizure disorders for which phenytoin is presently indicated.
合成了一系列(氟苄基)三唑并[4,5-c]吡啶,并测试了它们对啮齿动物最大电休克诱导惊厥的活性。最有前景的化合物14(BW 534U87)是嘌呤抗惊厥药的碳氮等排体,在啮齿动物中的表现表明14不会引起呕吐,可用于治疗目前使用苯妥英钠治疗的癫痫疾病。