SYNTHESIS OF 4-METHYLTHIO ANALOGS OF FLT AND AZT AND THEIR EVALUATION AGAINST HIV

被引：6

作者：

ABDELRAHMAN, AAH ^{[1
]}

ABDELBARY, HM ^{[1
]}

PEDERSEN, EB ^{[1
]}

NIELSEN, C ^{[1
]}

机构：

[1] STATENS SERUM INST,DEPT VIROL,RETROVIRUS LAB,DK-2300 COPENHAGEN,DENMARK

来源：

ARCHIV DER PHARMAZIE | 1995年 / 328卷 / 01期

关键词：

D O I：

10.1002/ardp.19953280112

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Silylated 4-methylthiouracil and 4-methylthiothymine were condensed in the presence of TMS triflate with methyl 2,3-dideoxy-3-fluoro-5-O-(4-phenylbenzoyl)-D-erythro-pentofuranoside (3) and methyl 3-azido-5-O (tert-butyldiphenylsilyl)-2,3-dideoxy-D-erythro-pentofuroside (8), respectively, to give the corresponding nucleosides which were deprotected. The 3'-azido nucleoside was reduced with triphenylphosphine to the corresponding 3'-amino nucleoside. The 3'-amino nucleoside was abo obtained by condensation of 4-methylthiothymidine with a 3-phthalimido sugar 14 followed by deprotection. The 4-methylthio analogue 11 of AZT showed moderate activity against HIV.

引用

页码：67 / 70

页数：4

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