Chapleo C B, Myers P L, Smith A C, Tulloch I F, Turner S, Walter D S
J Med Chem. 1987 May;30(5):951-4. doi: 10.1021/jm00388a038.
The synthesis and anticonvulsant activity of a number of 2-aryl-5-guanidino-1,3,4 thiadiazoles are described. The unsubstituted guanidine 2a was found to possess potent anticonvulsant properties; considerable reduction or loss of activity however was observed with the majority of the substituted guanidines. Incorporation of the guanidine group into an imidazoline ring also resulted in a loss of activity. Secondary pharmacological evaluation confirmed the anticonvulsant properties of 2a but also revealed that the compound exhibited a considerable degree of sedative activity.
描述了一系列2-芳基-5-胍基-1,3,4-噻二唑的合成及其抗惊厥活性。发现未取代的胍2a具有有效的抗惊厥特性；然而，大多数取代胍的活性显著降低或丧失。将胍基引入咪唑啉环也导致活性丧失。二级药理学评价证实了2a的抗惊厥特性，但也表明该化合物表现出相当程度的镇静活性。
