Anticonvulsant and Antiproteolytic Properties of 2,5-Disubstituted Oxadiazoles and Their Inhibition of Respiration in Rat Brain Homogenates
作者:Sunil K. Chaudhary、Sushil Kumar、Surendra S. Parmar、Mahima Chaudhary
DOI:10.1002/jps.2600670732
日期:1978.7
their sharp melting points, elemental analyses, and IR spectra, and evaluated for anticonvulsant activity. The protection afforded by oxadiazoles (100 mg/kg ip) against pentylenetetrazol (90 mg/kg sc)-induced convulsions ranged from 50 to 80%. All oxadiazoles inhibited the respiratory activity of rat brain homogenates during oxidation of pyruvate, alpha-ketoglutarate, and succinate. The presence of
合成了八种2-(3,4-亚甲基二氧基苯基)-5-芳基氨基1,3,4-恶二唑,其特征在于其敏锐的熔点,元素分析和红外光谱,并评估了其抗惊厥活性。恶二唑(100 mg / kg ip)对戊四氮(90 mg / kg sc)引起的惊厥的保护作用为50%至80%。所有的恶二唑类化合物在丙酮酸,α-酮戊二酸和琥珀酸的氧化过程中均抑制大鼠脑匀浆的呼吸活动。在丙酮酸的氧化过程中,向反应混合物中添加烟酰胺腺嘌呤二核苷酸(NAD)的存在降低了抑制程度。所有恶二唑均具有抗蛋白水解活性,这是由于它们减少胰蛋白酶诱导的牛血清白蛋白水解的能力所反映。这种抑制是浓度依赖性的,范围为10。0.5和1 mM的恶二唑分别为2至47.5和15.7至71.8%。所有恶二唑均竞争性抑制大鼠脑匀浆的体外琥珀酸脱氢酶活性。