SYNTHESIS AND BIOLOGICAL-ACTIVITY OF 8-OXADIHYDROPTERIDINES

被引：10

作者：

LIN, SC

HOLMES, GP

DUNN, DL

SKINNER, CG

机构：

[1] N TEXAS STATE UNIV,DEPT CHEM,DENTON,TX 76203

[2] TEXAS COLL OSTEOPATH MED,DENTON,TX 76203

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1979年 / 22卷 / 06期

关键词：

D O I：

10.1021/jm00192a024

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 6-substituted and 6, 7-disubstituted pyrimido(4, 5-b][l, 41oxazines (8-oxadihydropteridines) was synthesized through the condensation of an α-halo ketone and 2, 5-diamino-4, 6-pyrimidinediol. The resulting 8-oxadihydropteridines were assayed as potential antifolates in a dihydrofolate reductase enzyme system. The 2-amino-4-hydroxyoxadihydropteridines were found to possess greater biological activity than the corresponding 2.4-diamino compounds.The pteroic acid homeostere 2-amino-4-hydroxy-6-phenethyl-8-oxadihydropteridine was the most potent of the compounds tested. © 1979, American Chemical Society. All rights reserved.

引用

页码：741 / 743

页数：3

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