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Highly potent inhibitors of TNF-alpha production. Part I: discovery of new chemical leads and their structure-activity relationships |
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| Authors: | Matsui Toshiaki Kondo Takashi Nishita Yoshitaka Itadani Satoshi Nakatani Shingo Omawari Nagashige Sakai Masaru Nakazawa Shuichi Ogata Akihito Mori Hideaki Terai Kouichiro Kamoshima Wataru Ohno Hiroyuki Obata Takaaki Nakai Hisao Toda Masaaki |
| Institution: | Fukui Research Institute, Ono Pharmaceutical Co., Ltd., Technoport, Yamagishi, Mikuni, Sakai, Fukui, Japan. to.matsui@ono.co.jp |
| Abstract: | Discovery of new chemical leads of inhibitors for TNF-alpha production starting from the chemical modification of 1 is reported. Further biological studies of 1 to disclose the site of its action strongly suggested that 1 inhibits LPS-induced TNF-alpha expression in the liver and spleen of mice. Structure-activity relationships (SARs) are also discussed and full details including the chemistry are reported. |
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