title: Expedient solid-phase synthesis of both symmetric and asymmetric diol libraries targeting aspartic proteases.
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.
authors.affiliation: Department of Chemistry, National University of Singapore, Singapore.
authors.forename: Haibin
authors.initials: H
authors.lastname: Shi
authors.forename: Kai
authors.initials: K
authors.lastname: Liu
authors.forename: Wendy W Y
authors.initials: WW
authors.lastname: Leong
authors.forename: Shao Q
authors.initials: SQ
authors.lastname: Yao