期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 17, 期 20, 页码 5614-5619出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.07.095
关键词
HIV-1 protease inhibitor; C-2 symmetry; sulfoximine; transition state mimic
Based on the unique property of sulfoximine and the homodimeric Q structural symmetry of HIV-1 protease, a novel class of sulfoximine-based pseudosymmetric HIV-1 protease inhibitors was designed and synthesized. The sulfoximine moiety was demonstrated to be important for HIV-1 protease inhibitor potency. The most active stereoisomer (2S,2 ' S) displays a potency of 2.5 nM (IC50) against HIV-1 protease and an anti-HIV-1 activity of 408 nM (IC50). A possible mode of action is proposed. (c) 2007 Elsevier Ltd. All rights reserved.
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