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Highly potent inhibitors of TNF-alpha production. Part I: discovery of new chemical leads and their structure-activity relationships. 2002
Toshiaki Matsui, and
Takashi Kondo, and
Yoshitaka Nishita, and
Satoshi Itadani, and
Shingo Nakatani, and
Nagashige Omawari, and
Masaru Sakai, and
Shuichi Nakazawa, and
Akihito Ogata, and
Hideaki Mori, and
Kouichiro Terai, and
Wataru Kamoshima, and
Hiroyuki Ohno, and
Takaaki Obata, and
Hisao Nakai, and
Masaaki Toda
Fukui Research Institute, Ono Pharmaceutical Co., Ltd., Technoport, Yamagishi, Mikuni, Sakai, Fukui, Japan. to.matsui@ono.co.jp
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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