140196-57-2Relevant articles and documents
Expedient solid-phase synthesis of both symmetric and asymmetric diol libraries targeting aspartic proteases
Shi, Haibin,Liu, Kai,Leong, Wendy W.Y.,Yao, Shao Q.
supporting information; experimental part, p. 3945 - 3948 (2010/03/30)
C2-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 (Ki = 400 nM) against HIV-1 protease.