Highly potent inhibitors of TNF-α production. Part II: Metabolic stabilization of a newly found chemical lead and conformational analysis of an active diastereoisomer

Abstract 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.