Design, synthesis, and biological evaluation of novel coxsackievirus B3 inhibitors

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• 作者：Michal Š ; á ; la ; Arm ; o M. De Palma ; Hubert Hř ; ebabecký ; Radim Nencka ; Martin Drač ; í ; nský ; Pieter Leyssen ; Johan Neyts ; Antoní ; n Holý
• 关键词：6-Chloropurine ; Coxsackievirus B3 ; Mitsunobu reaction ; Bicyclo[2.2.1]heptane ; Fluorination
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2010
• 出版时间：15 June 2010
• 年：2010
• 卷：18
• 期：12
• 页码：4374-4384
• 全文大小：2082 K

文摘

The synthesis and SAR study of a novel class of coxsackievirus B3 (CVB3) inhibitors are reported. These compounds could be considered as the 6-chloropurines substituted at position 9 with variously substituted bicyclic scaffolds (bicyclo[2.2.1]heptane/ene—norbornane or norbornene). The synthesis and biological evaluation of 31 target compounds are described. Several of the analogues inhibited CVB3 in the low micromolar range (0.66–2 μM). Minimal or no cytotoxicity was observed.