Synthesis and Biological Evaluation of 7-Deoxy Analogues of the Human Rhinovirus 3C Protease Inhibitor Thysanone
作者:Katrin Schünemann、Daniel P. Furkert、Stephen Connelly、John D. Fraser、Jonathan Sperry、Margaret A. Brimble
DOI:10.1002/ejoc.201301515
日期:2014.1
The synthesis of (±)-7-deoxythysanone and three analogues has been developed. The key oxa-Pictet–Spengler reaction enabled the synthesis of the naphthopyran precursor, which could be readily converted to 7-deoxythysanone and three related analogues. The biological activity of these compounds was also evaluated against HRV 3C protease, the results of which suggest that inhibition of the enzyme requires
(±)-7-deoxythysanone 和三个类似物的合成已经开发出来。关键的 oxa-Pictet-Spengler 反应能够合成萘并吡喃前体,该前体可以很容易地转化为 7-脱氧麝香酮和三种相关的类似物。还针对 HRV 3C 蛋白酶评估了这些化合物的生物活性,其结果表明酶的抑制需要 7-oxa 功能的存在。