Highly potent inhibitors of TNF-α production. Part I: Discovery of new chemical leads and Their structure–Activity relationships

…, S Nakatani, N Omawari, M Sakai, S Nakazawa…

Index: 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 Bioorganic and Medicinal Chemistry, 2002 , vol. 10, # 12 p. 3757 - 3786

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Citation Number: 14

Abstract

Discovery of new chemical leads of inhibitors for TNF-α 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-α expression in the liver and spleen of mice. Structure–activity relationships (SARs) are also discussed and full details including the chemistry are reported.