二氢叶酸还原酶抑制剂:5-取代苯硫基(硒基)-2,4-二氨基嘧啶类化合物的合成和抑酶活性

According to the principle of isosterism the-CH₂-group of 5-(substituted benzyl)-2, 4-diaminopyrimidine was modified by—S—and—Se—and some 5-(substituted phenyl)thio-2, 4-diaminopyrimidines and 5-(substituted phenyl)seleno-2,4-diaminopyrimidines were synthesized. Their inhibitory activities on L. casei and chicken liver dihydrofolate reductase were determined. Preliminary data showed that the inhibitory activities of these compounds were less than those of the corresponding 5-(substituted benzyl)-2, 4-diaminopyrimidines. Their selectivities are also decreased.

STUDIES ON THE SYNTHESIS OF DIHYDROFOLATE REDUCTASE INHIBITOR,5-(SUBSTITUTED PHENYL)-THIO(SELENO)-2,4-DIAMINOPYRIMIDINES AND THEIR INHIBITORY ACTIVITY TO L.CASEI AND CHICKEN LIVER DHFR

According to the principle of isosterism the-CH₂-group of 5-(substituted benzyl)-2, 4-diaminopyrimidine was modified by—S—and—Se—and some 5-(substituted phenyl)thio-2, 4-diaminopyrimidines and 5-(substituted phenyl)seleno-2,4-diaminopyrimidines were synthesized. Their inhibitory activities on L. casei and chicken liver dihydrofolate reductase were determined. Preliminary data showed that the inhibitory activities of these compounds were less than those of the corresponding 5-(substituted benzyl)-2, 4-diaminopyrimidines. Their selectivities are also decreased.