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ID: ALA1137472
Journal: Bioorg Med Chem Lett
Title: Discovery of potent HIV-1 protease inhibitors incorporating sulfoximine functionality.
Authors: Lu D, Vince R.
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.
CiteXplore: 17822899