ovalbumin and etiprednol-dicloacetate

Loteprednol etabonate (LE) is the first, highly successful soft corticosteroid (SC) designed using the 'inactive metabolite' approach, starting with ∆. The new 6α, 9α, 16α and β 17α-dichloroacetyl 17β-esters were synthesized from the correspondingly substituted ∆. The 6α or 9α-fluoro substitution produced highly potent corticosteroids, but the 17α-dichloroacetyl substituent provided 'softness' in all cases. Local application of these steroids will significantly reduce systemic activity, due to the facile hydrolytic deactivation of these molecules.. A 17α-dichloroacetyl derivative of fluticasone (FLU) is highly potent but much safer than the currently used propionate or furoate ester.

Topics: Adrenal Cortex Hormones; Animals; Anti-Inflammatory Agents; Disease Models, Animal; Fluticasone; Lipopolysaccharides; Loteprednol Etabonate; Male; Ovalbumin; Rats; Rats, Inbred BN; Structure-Activity Relationship; Tumor Necrosis Factor-alpha