SYNTHESIS AND ANTI-VIRAL ACTIVITY OF SOME PHOSPHATES OF BROAD-SPECTRUM ANTI-VIRAL NUCLEOSIDE, 1-BETA-D-RIBOFURANOSYL-1,2,4-TRIAZOLE-3-CARBOXAMIDE (RIBAVIRIN)

被引：40
|
作者：
ALLEN, LB
BOSWELL, KH
KHWAJA, TA
MEYER, RB
SIDWELL, RW
WITKOWSKI, JT
CHRISTENSEN, LF
ROBINS, RK
机构：
[1] BRIGHAM YOUNG UNIV, DEPT CHEM, PROVO, UT 84602 USA
[2] ICN PHARMACEUT INC, IRVINE, CA 92664 USA
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 1978年 / 21卷 / 08期
关键词：
D O I：
10.1021/jm00206a005
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
1-.beta.-D-Ribofuranosyl-1,2,4-triazole-3-carboxamide 5''-phosphate was prepared and converted into the following derivatives: the 5''-phosphoramidate, the 5''-diphosphate, the 5''-triphosphate and the cyclic 3'',5''-phosphate. The cyclic 2'',3''-phosphate was prepared from the parent nucleoside, 1-.beta.-D-ribofuranosyl-1,2,4-triazole-3-carboxamide and was opened to the 2''(3'')-phosphate. These compounds exhibited significant antiviral activity against several viruses in cell culture. Ribovirin 5''-phosphate was effective when tested against lethal infections in mice caused by influenza A2, influenza B and murine hepatitis viruses.
引用
收藏
页码：742 / 746
页数：5
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