Expedient solid-phase synthesis of both symmetric and asymmetric diol libraries targeting aspartic proteases.
作者： Haibin Shi , Kai Liu , Wendy W.Y. Leong , Shao Q. Yao
DOI: 10.1016/J.BMCL.2009.03.041
关键词:
摘要: Abstract C2-symmetric diols have been shown to be highly potent against HIV-1 protease (PR). However, gaining access these compounds has hampered by the need of multistep solution-phase reactions which are often tedious and inefficient. In this Letter, we disclosed a solid-phase strategy for rapid preparation small molecule-based, symmetric asymmetric as potential inhibitors. Upon biological screening, found one them, SYM-5, selective inhibitor (Ki = 400 nM) protease.
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