荧光1,2,4-噻二唑-3,5-二酮衍生物的合成及其对精子的标记作用

Synthesis of Fluorescent 1,2,4-Thiadiazole-3,5-diones and Their Labeling Effect on Sperm

合成了3个含有荧光基团的1,2,4-噻二唑-3,5-二酮衍生物,其结构经^(1)H NMR,^(13)C NMR,HR-MS(ESI)表征,并考察了这些衍生物对精子的制动活性和荧光标记作用。结果表明:与先导化合物Tideglusib相比,目标化合物均保持了较强的杀精活性,且在紫外光激发下,具有相似的荧光标记模式。

Three fluorescent 1,2,4-thiadiazole-3,5-diones were synthesized and their structures were characterized by ^(1)H NMR,^(13)C NMR and HR-MS(ESI).The spermostatic activity and sperm staining activity of target compounds were investigated as well.The results indicated that compared with the leading compound Tideglusib,three compounds kept spermicide activity.All the compounds have similar fluorescent labeling position in human sperm under excitation of ultraviolet.