Discovery of novel phosphonic acid derivatives as new chemical leads for inhibitors of TNF-α production

…, S Takahashi, N Matsunaga, K Nakamura…

Index: Matsui, Toshiaki; Takahashi, Shinya; Matsunaga, Naoki; Nakamura, Kazunori; Omawari, Nagashige; Sakai, Masaru; Kamoshima, Wataru; Terai, Kouichiro; Ohno, Hiroyuki; Obata, Takaaki; Nakai, Hisao; Toda, Masaaki Bioorganic and Medicinal Chemistry, 2002 , vol. 10, # 12 p. 3807 - 3815

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Citation Number: 11

Abstract

2-(Acylamino) benzylphosphonic acid 6 derived from an artificial substrate of sphingomyelinase was found to show inhibitory activity of TNF-α 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-α production is reported.