Design, Synthesis, and Antiviral Evaluation of Purine-尾-lactam and Purine-aminopropanol Hybrids

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• 作者：Matthias D鈥檋ooghe ; Karen Mollet ; Rob De Vreese ; Tim H. M. Jonckers ; G茅ry Dams ; Norbert De Kimpe
• 刊名：Journal of Medicinal Chemistry
• 出版年：2012
• 出版时间：June 14, 2012
• 年：2012
• 卷：55
• 期：11
• 页码：5637-5641
• 全文大小：238K
• 年卷期：v.55,no.11(June 14, 2012)
• ISSN：1520-4804

文摘

Purine-尾-lactam chimera were prepared as a novel class of hybrid systems through N-alkylation of 6-benzylamino- or 6-benzyloxypurine with (蠅-haloalkyl)-尾-lactams, followed by reductive ring opening of the 尾-lactam ring by LiEt₃BH to provide an entry into the class of purine-aminopropanol hybrids. Both new types of hybrid systems were assessed for their antiviral activity and cytotoxicity, resulting in the identification of eight purine-尾-lactam hybrids and two purine-aminopropanol hybrids as promising lead structures.