Pandey B R, Parmar S S, Kumar S, Brumleve S J
Pharmacology. 1978;16(6):344-8. doi: 10.1159/000136790.
Nine 1-(3,4-dimethoxyphenylethyl)-2-methyl-4-(substituted benzylidene)-5-imidazolones were synthesized, characterized by their sharp melting points, elemental analyses and infrared spectra and evaluated for anticonvulsant activity. All 1,2,4-trisubstituted-5-imidazolones at a dose of 100 mg/kg i.p. possessed anticonvulsant activity and the degree of protection observed against pentylenetetrazol-induced convulsions in mice ranged from 20 to 60%. These 1,2,4-trisubstituted-5-imidazolones selectively inhibited in vitro oxidation of the nicotinamide adenine dinucleotide (NAD)-dependent oxidation of pyruvate, alpha-ketoglutarate and NADH by rat brain homogenates while the NAD-independent oxidation of succinate remained unaltered. The anti-convulsant activity possessed by 1,2,4-trisubstituted-5-imidazolones was unrelated with their ability to selectively inhibit respiratory activity of rat brain homogenates.
合成了9种1-(3,4-二甲氧基苯乙基)-2-甲基-4-(取代亚苄基)-5-咪唑酮，通过其熔点、元素分析和红外光谱对其进行了表征，并对其抗惊厥活性进行了评估。所有1,2,4-三取代-5-咪唑酮腹腔注射剂量为100mg/kg时均具有抗惊厥活性，在小鼠中观察到的对戊四氮诱导惊厥的保护程度为20%至60%。这些1,2,4-三取代-5-咪唑酮在体外选择性抑制大鼠脑匀浆中烟酰胺腺嘌呤二核苷酸（NAD）依赖性的丙酮酸、α-酮戊二酸和NADH的氧化，而琥珀酸的非NAD依赖性氧化则保持不变。1,2,4-三取代-5-咪唑酮所具有的抗惊厥活性与其选择性抑制大鼠脑匀浆呼吸活性的能力无关。
