Summary
Novelty: Novel phenoxyalkylcarboxylic acid derivatives, said to have strong and selective leukotriene (LT) antagonistic action, are disclosed. These compounds may be useful for the prevention and treatment of allergic diseases such as asthma. Processes for preparing these carboxylic acid derivatives are described.
Biology: The effects of the exemplified compound on leukotriene D4-induced bronchoconstriction in guinea pigs was evaluated. Bronchoconstriction was inhibited by 71% at a dose of 1 mg/kg iv. The compounds also showed strong antagonistic action to leukotriene D4 in the isolated guinea pig trachea.
Chemistry: Synthesis of the compounds is described in seven examples, including 4[3[3-(4-acetyl-3-hydroxy-2-propylphenylthio)propxy]-6-1(-hydroxyethyl)-2-propylphenoxy]butanoic acid.
Structure: