发明名称 USE OF DIARYLACETIC ACID HYDRAZIDE DERIVATIVES AS ANTICONVULSIVE AGENTS
摘要 FIELD: organic chemistry. SUBSTANCE: products: acyclic compounds, hydrazides of diphenylacetic, benzylic and bis-(o-tolyl)-glycolic acids of the general formula (1a-c):where: R= R- H (1a); R- OH, R- H (1b); R- OH, R- CH(1c). These compounds are colorless, crystalline, soluble in usual organic solvents substances exhibiting the following m. p. values: 136-137 C (1a); 168-169 C (1b); 163-164 C (1c), and yields - 94%, 88% and 66%, respectively. Synthesized compounds show the following anticonvulsive activity (by maximal electroshock assay): for compound (1a) - ED54 (31-78 mg/kg); for 1b - ED37 (28-48 mg/kg, and for 1c - ED35 (33-38 mg/kg). Acute toxicity expressed as LDvalues: 520 (486-568), 740 (688-705) and 680 (621-745) mg/kg, respectively. EFFECT: improved method of synthesis, enhanced effectiveness.
申请公布号 RU94023764(A) 申请公布日期 1997.05.10
申请号 RU19940023764 申请日期 1994.06.23
申请人 PERMSKIJ FARMATSEVTICHESKIJ INSTITUT 发明人 KOZ'MINYKH E.N.;BEREZINA E.S.;KOZ'MINYKH V.O.;KOLLA V.EH.;SHELENKOVA S.A.;JAKOVLEV I.B.
分类号 A61K31/15;A61P25/08;C07C241/04 主分类号 A61K31/15
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