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Sphingomyelin analogues as inhibitors of sphingomyelinase |
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| Authors: | Taguchi Minoru Sugimoto Kikuo Goda Ken-ichi Akama Tomoko Yamamoto Kyoko Suzuki Taizo Tomishima Yasumitsu Nishiguchi Mariko Arai Koshi Takahashi Kenzo Kobori Takeo |
| Affiliation: | Medicinal 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 |
| 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. |
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