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  • Title: Synthesis and evaluation of novel phosphate ester analogs as neutral sphingomyelinase inhibitors.
    Author: Imagawa H, Oda M, Takemoto T, Yamauchi R, Yoshikawa T, Yamamoto H, Nishizawa M, Takahashi H, Hashimoto M, Yabiku K, Nagahama M, Sakurai J.
    Journal: Bioorg Med Chem Lett; 2010 Jul 01; 20(13):3868-71. PubMed ID: 20627555.
    Abstract:
    A novel sphingomyelin inhibitor RY221B-a, which contains a bipyridyl moiety as a metal coordination site was designed based upon the mechanism of phosphate ester hydrolysis. RY221B-a was synthesized from N-Boc-sphingosine in three steps via selective etherification using stannyl acetal. Synthesized RY221B-a exhibited relatively-strong inhibitory activity against Bc-SMase (IC(50)=1.2microM).
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