Expedient solid-phase synthesis of both symmetric and asymmetric diol libraries targeting aspartic proteases

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
Appears in Collections:	Staff Publications

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