Synthesis and In-vitro Activity of 4′-Modified Analogues of ddA as Potent Anti-HIV Agents

被引:3
|
作者
Hong, Joon Hee [2 ]
Oh, Chang Hyun [1 ]
机构
[1] Korea Inst Sci & Technol, Biomat Chem Res Ctr, Seoul 136791, South Korea
[2] Chosun Univ, Coll Pharm, Project Team BK 21, Kwangju 501759, South Korea
关键词
Antiviral agents; Deoxythreosyl C-Nucleoside; Ozonolysis; Phosphorylation; ISOMERIC DIDEOXYNUCLEOSIDES; 9-DEAZAADENOSINE; NUCLEOSIDES;
D O I
10.1002/ardp.200900063
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
This paper reports the synthesis of novel 4'-hydrophobic pocket deoxythreosyl C-nucleosides. The key threose-like intermediates 9 and 14 were constructed from acyclic ketone derivatives, respectively. The antiviral activities of the synthesized compounds against the HIV-1, HSV-1, HSV-2, and HCMV viruses were evaluated. The 9-deaza-adenine derivatives 10 and 20 showed good anti-HIV activity without exhibiting significant cytotoxicity.
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页码:600 / 604
页数:5
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