SYNTHESIS OF NUCLEOSIDES AND RELATED-COMPOUNDS - SYNTHESIS AND ANTI-HIV ACTIVITY OF 9-[C-4,T-5-BIS(HYDROXYMETHYL)CYCLOPENT-2-EN-R-1-YL]-9H-ADENINE

被引：69

作者：

KATAGIRI, N ^{[1
]}

NOMURA, M ^{[1
]}

SATO, H ^{[1
]}

KANEKO, C ^{[1
]}

YUSA, K ^{[1
]}

TSURUO, T ^{[1
]}

机构：

[1] JAPANESE FDN CANC RES,CTR CANC CHEMOTHERAPY,TOSHIMA KU,TOKYO 170,JAPAN

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1992年 / 35卷 / 10期

关键词：

D O I：

10.1021/jm00088a026

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and in vitro anti-HIV activity of two new racemic nucleoside analogues are described; namely, 9-[c-4,t-5-bis(hydroxymethyl)cyclopent-2-en-r-1-yl]-9H-adenine (12) and its guanine analogue 18. While the latter (18) showed no activity, the therapeutic index of the former (12) was 200 and comparable to that (400) of carbovir. One enantiomer of 12 may be viewed as an analogue of carbocyclic oxetanocin and the other as an analogue of carbovir. Hence, these results indicate that one or both of the individual enantiomers of 12 could serve as candidates or lead compounds for the development of anti-AIDS agents.

引用

页码：1882 / 1886

页数：5

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