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Sphingomyelin analogues as inhibitors of sphingomyelinase
Minoru Taguchi1, Kikuo Sugimoto, Ken-ichi Goda
1Medicinal Research Laboratories, Taisho Pharmaceutical Co., Ltd., 1-403 Yoshino-cho, Kita-ku, Saitama-shi, 331-9530, Saitama, Japan. minoru.taguchi@po.rd.taisho.co.jp
Bioorganic & Medicinal Chemistry Letters
|June 5, 2003
Abstract:
To search for neutral sphingomyelinase inhibitors we designed and synthesized hydrolytically stable analogues of sphingomyelin. The novel compounds 8 and 9 which were replaced the phosphodiester moiety of sphingomyelin with the carbamate moiety showed inhibitory activity with an IC(50) value of micro M on neutral sphingomyelinase in rat brain microsomes. Compound 8i showed a selective neutral sphingomyelinase inhibitory activity.