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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. [Copyright &y& Elsevier]

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. [Copyright &y& Elsevier]

Design and synthesis of metabolically stabilized inhibitors of TNF-α production, which could be new drug candidates, are reported. Conformational analysis of an active diastereoisomer was performed based on biological evaluations of the conformationally fixed indane derivatives 17 and 18. Structure–activity relationships (SARs) based on biological evaluations of the optically active derivatives are also discussed. Full details including chemistry are reported. [Copyright &y& Elsevier]

The discovery of 2-acylamino-2-phenylethyl disodium phosphates and as structurally novel inhibitors of TNF-α production is reported. Structure–activity relationships (SARs) are also discussed. [Copyright &y& Elsevier]