4.3 Article

Design and synthesis of new 2-substituted-5-[2-(2-halobenzyloxy)phenyl]-1,3,4-oxadiazoles as anticonvulsant agents

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CHEMICAL & PHARMACEUTICAL BULLETIN
卷 56, 期 4, 页码 509-512

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PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.56.509

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benzodiazepine receptor; 1,3,4-oxadiazole; anticonvulsant; structure-activity relationship (SAR)

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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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