Document Report Card
Basic Information
ID: ALA1153582
Journal: Bioorg Med Chem Lett
Title: Expedient solid-phase synthesis of both symmetric and asymmetric diol libraries targeting aspartic proteases.
Authors: Shi H, Liu K, Leong WW, Yao SQ.
Abstract: C(2)-symmetric diols have been shown to be highly potent against HIV-1 protease (PR). However, gaining access to these compounds has been hampered by the need of multistep solution-phase reactions which are often tedious and inefficient. In this Letter, we have disclosed a solid-phase strategy for rapid preparation of small molecule-based, symmetric and asymmetric diols as potential HIV-1 protease inhibitors. Upon biological screening, we found one of them, SYM-5, to be a potent and selective inhibitor (K(i)=400 nM) against HIV-1 protease.
CiteXplore: 19328682