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  • Title: Expedient solid-phase synthesis of both symmetric and asymmetric diol libraries targeting aspartic proteases.
    Author: Shi H, Liu K, Leong WW, Yao SQ.
    Journal: Bioorg Med Chem Lett; 2009 Jul 15; 19(14):3945-8. PubMed ID: 19328682.
    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.
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