Please use this identifier to cite or link to this item: https://doi.org/10.1016/j.bmcl.2009.03.041
Title: Expedient solid-phase synthesis of both symmetric and asymmetric diol libraries targeting aspartic proteases
Authors: Shi, H.
Liu, K.
Leong, W.W.Y.
Yao, S.Q. 
Keywords: Combinatorial chemistry
Drug discovery
Protease inhibitor
Solid-phase synthesis
Issue Date: 15-Jul-2009
Citation: Shi, H., Liu, K., Leong, W.W.Y., Yao, S.Q. (2009-07-15). Expedient solid-phase synthesis of both symmetric and asymmetric diol libraries targeting aspartic proteases. Bioorganic and Medicinal Chemistry Letters 19 (14) : 3945-3948. ScholarBank@NUS Repository. https://doi.org/10.1016/j.bmcl.2009.03.041
Abstract: 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. © 2009 Elsevier Ltd. All rights reserved.
Source Title: Bioorganic and Medicinal Chemistry Letters
URI: http://scholarbank.nus.edu.sg/handle/10635/93783
ISSN: 0960894X
DOI: 10.1016/j.bmcl.2009.03.041
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