期刊
CHEMICAL & PHARMACEUTICAL BULLETIN
卷 56, 期 4, 页码 509-512出版社
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.56.509
关键词
benzodiazepine receptor; 1,3,4-oxadiazole; anticonvulsant; structure-activity relationship (SAR)
Anew series of 2-substituted-5-[2-(2-halobenzyloxy)phenyl]-1,3,4-oxadiazoles was designed and synthesized as anticonvulsant agents. Electroshock and pentylenetetrazole-induced lethal convulsion tests showed that the introduction of an amino group at position 2 of 1,3,4-oxadiazole ring and a fluoro substituent at ortho position of benzyloxy moiety had the best anticonvulsant activity. Our results showed that this effect is mediated through benzodiazepine receptors mechanism.
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