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

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]