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  • Title: Spirodiketopiperazine-based CCR5 antagonists: Lead optimization from biologically active metabolite.
    Author: Nishizawa R, Nishiyama T, Hisaichi K, Matsunaga N, Minamoto C, Habashita H, Takaoka Y, Toda M, Shibayama S, Tada H, Sagawa K, Fukushima D, Maeda K, Mitsuya H.
    Journal: Bioorg Med Chem Lett; 2007 Feb 01; 17(3):727-31. PubMed ID: 17118654.
    Abstract:
    Hydroxylated derivatives were designed and synthesized based on the information of oxidative metabolites. Compounds derived from beta-substituted (2R,3R)-2-amino-3-hydroxypropionic acid showed improved inhibitory activities against the binding of MIP-1alpha to human CCR5, compared with the non-hydroxylated derivatives and the other isomers.
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