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Synthesis and evaluation of novel phosphate ester analogs as neutral sphingomyelinase inhibitors |
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| Authors: | Hiroshi Imagawa Masataka Oda Takayuki Takemoto Rieko Yamauchi Tomomi Yoshikawa Hirofumi Yamamoto Mugio Nishizawa Hironobu Takahashi Manabu Hashimoto Kenta Yabiku Masahiro Nagahama Jun Sakurai |
| Institution: | 1. Faculty of Pharmaceutical of Sciences, Tokushima Bunri University, Tokushima, Japan;2. Institute of Pharmacognosy, Tokushima Bunri University, Tokushima, Japan |
| 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 (IC50 = 1.2 μM). |
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