Chaudhary M, Parmar S S, Chaudhary S K, Chaturvedi A K, Sastry B V
J Pharm Sci. 1976 Mar;65(3):443-6. doi: 10.1002/jps.2600650336.
Several 1-aryl-3-(2-pyrimidyl)thiocarbamides and their corresponding cyclized 2-arylimino-3-(2-pyrimidyl)thiazolid-4-ones were synthesized and characterized by their sharp melting points and elemental analyses. These thiocarbamides and 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 was unrelated to their ability to inhibit the respiratory activity of rat brain homogenates during oxidation of sodium pyruvate. Cyclization of thiocarbamides to the corresponding thiazolidones in general enhanced their CNS depressant and enzyme inhibitory effectiveness.
合成了几种1-芳基-3-(2-嘧啶基)硫代氨基甲酰胺及其相应的环化产物2-芳基亚氨基-3-(2-嘧啶基)噻唑烷-4-酮，并通过其尖锐的熔点和元素分析对其进行了表征。这些硫代氨基甲酰胺和噻唑烷酮对戊四氮诱导的惊厥具有抗惊厥活性，并增强了小鼠戊巴比妥诱导的催眠作用。这些硫代氨基甲酰胺和噻唑烷酮中的大多数选择性地抑制烟酰胺腺嘌呤二核苷酸(NAD)依赖性的丙酮酸氧化，而另一方面，添加NAD的使用则保持不变。硫代氨基甲酰胺和噻唑烷酮的抗惊厥活性与其在丙酮酸氧化过程中抑制大鼠脑匀浆呼吸活性的能力无关。一般来说，硫代氨基甲酰胺环化为相应的噻唑烷酮会增强其对中枢神经系统的抑制作用和酶抑制效果。
