doi: 10.1016/j.bmcl.2007.07.095.
Epub 2007 Aug 23.
Discovery of potent HIV-1 protease inhibitors incorporating sulfoximine functionality
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- PMID: 17822899
- DOI: 10.1016/j.bmcl.2007.07.095
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Discovery of potent HIV-1 protease inhibitors incorporating sulfoximine functionality
Bioorg Med Chem Lett.
.
Erratum in
- Bioorg Med Chem Lett. 2008 Mar 15;18(6):2228
Abstract
Based on the unique property of sulfoximine and the homodimeric C(2) 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 (IC(50)) against HIV-1 protease and an anti-HIV-1 activity of 408 nM (IC(50)). A possible mode of action is proposed.
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