CNS Depressant Activity of Pyrimidylthiazolidones and their Selective Inhibition of NAD‐Dependent Pyruvate Oxidation
作者:Mahima Chaudhary、Surendra S. Parmar、Sunil K. Chaudhary、Arvind K. Chaturvedi、B.V. Rama Sastry
DOI:10.1002/jps.2600650336
日期:1976.3
thiazolidones possessed anticonvulsant activity against pentylenetetrazol-induced convulsions and potentiated pentobarbital-induced hypnosis in mice. Most of these thiocarbamides and thiazolidones selectively inhibited nicotinamide adenine dinucleotide (NAD)-dependent oxidation of pyruvate, where the use of added NAD dether hand, remained unaltered. The anticonvulsant activity of thiocarbamides and thiazolidones
合成了几种1-芳基-3-(2-嘧啶基)硫代氨基甲酸酯及其相应的环化2-芳基氨基-3-(2-嘧啶基)噻唑烷-4-酮,并通过其敏锐的熔点和元素分析对其进行了表征。这些硫脲和噻唑烷酮具有抗戊戊四唑诱发的惊厥和增强的戊巴比妥诱发的催眠作用。这些硫代碳酰胺和噻唑烷酮中的大多数选择性地抑制了烟酰胺腺嘌呤二核苷酸(NAD)依赖性的丙酮酸氧化,而使用添加的NAD鹿角手仍保持不变。硫脲和噻唑烷酮的抗惊厥活性与它们在丙酮酸钠氧化过程中抑制大鼠脑匀浆的呼吸活性的能力无关。