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Discovery of novel phosphonic acid derivatives as new chemical leads for inhibitors of TNF-alpha production |
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| Authors: | Matsui Toshiaki Takahashi Shinya Matsunaga Naoki Nakamura Kazunori Omawari Nagashige Sakai Masaru Kamoshima Wataru Terai Kouichiro Ohno Hiroyuki Obata Takaaki Nakai Hisao Toda Masaaki |
| Affiliation: | Fukui Research Institute, Ono Pharmaceutical Co., Ltd., Yamagishi, Mikuni, Sakai, Fukui, Japan. to.matsui@ono.co.jp |
| Abstract: | 2-(Acylamino)benzylphosphonic acid 6 derived from an artificial substrate of sphingomyelinase was found to show inhibitory activity of TNF-alpha production. Structural optimization was started with the chemical modification of 6. The discovery of another chemical leads 7, 8, 10 and 16 for the development of structurally new inhibitors of TNF-alpha production is reported. |
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