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

@article{Matsui2002DiscoveryON,
  title={Discovery of novel phosphonic acid derivatives as new chemical leads for inhibitors of TNF-alpha production.},
  author={Toshiaki Matsui and Shinya Takahashi and Naoki Matsunaga and Kazunori Nakamura and Nagashige Omawari and Masaru Sakai and Wataru Kamoshima and Kouichiro Terai and Hiroyuki Ohno and Takaaki Obata and Hisao Nakai and Masaaki Toda},
  journal={Bioorganic & medicinal chemistry},
  year={2002},
  volume={10 12},
  pages={3807-15}
}
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.