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1-（氟苄基）-4-氨基-1H-1,2,3-三唑并[4,5-c]吡啶：合成与抗惊厥活性

1-(Fluorobenzyl)-4-amino-1H-1,2,3-triazolo[4,5-c]pyridines: synthesis and anticonvulsant activity.

作者信息

Kelley J L, Koble C S, Davis R G, McLean E W, Soroko F E, Cooper B R

机构信息

Division of Organic Chemistry, Burroughs Wellcome Co., Research Triangle Park, North Carolina 27709, USA.

出版信息

J Med Chem. 1995 Sep 29;38(20):4131-4. doi: 10.1021/jm00020a030.

DOI:10.1021/jm00020a030
PMID:7562950
Abstract

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.

摘要

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。