Patent Evaluation: Novel di-t-butylphenol Amides as 5-lipoxygenase Inhibitors

Summary

Novelty: Anti-allergic properties are claimed for (substituted)-di-t-butylphenols having LT-synthesis inhibitory activity.

Biology: Although in vitro and in vivo tests are described, no specific details for the compounds are provided. The preferred compounds are claimed to have ED₄₀ < 25 mg/kg in the guinea pig bronchoconstriction assay and one compound is stated to be orally active.

Chemistry: There are thirty-two synthetic examples with many compounds tabulated. A typical specifically claimed compound (among fourteen) is 5-[3-(3,5-di-t-butyl-4-hydroxybenzamido)phenyl]-tetrazole.

Structure: