Synthesis and anti-HIV activity of 9-[c-4,t-5-bis(hydroxymethyl)cyclopent-2-en-r-1-yl]-9H-adenine.
Synthesis and anti-HIV activity of 9-[c-4,t-5-bis(hydroxymethyl)cyclopent-2-en-r-1-yl]-9H-adenine.
复制标题
9-[c-4,t-5-双(羟甲基)环戊-2-en-r-1-基]-9H-腺嘌呤的合成和抗HIV活性。
DOI：
10.1021/jm00088a026
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发表时间：
1992
影响因子：
7.3
通讯作者：
T. Tsuruo
中科院分区：
文献类型：
--
作者：
N. Katagiri;M. Nomura;H. Satō;C. Kaneko;K. Yusa;T. Tsuruo
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.
