Gilead Sciences & IOCB Research Centre, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, Prague, Czech Republic.
Bioorg Med Chem. 2010 Jun 15;18(12):4374-84. doi: 10.1016/j.bmc.2010.04.081. Epub 2010 Apr 29.
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 (0.66-2muM). Minimal or no cytotoxicity was observed.
报告了一类新型柯萨奇病毒 B3（CVB3）抑制剂的合成和构效关系研究。这些化合物可以被认为是 9 位取代的 6-氯嘌呤，取代基为各种取代的双环支架（二环[2.2.1]庚烷/烯-降冰片烷或降冰片烯）。描述了 31 个目标化合物的合成和生物学评价。一些类似物在低微摩尔范围内抑制 CVB3（0.66-2μM）。观察到最小或无细胞毒性。
