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Summary
Novelty: Styryl compounds having potential leukotriene, cyclooxygenase, 5-lipoxygenase and histamine inhibitory activity are disclosed. Compounds of the invention are potentially useful for the prevention and treatment of a wide range of inflammatory and allergic disorders. These include bronchial asthma, chronic bronchitis, coronary vascular diseases and gastrointestinal ulceration.
Biology: In vitro evaluation of guinea pig ileum contraction (induced by leukotriene D4) inhibition is described. The most potent test compound (D) gave an IC50 value of 6.6 × 10−11 g/ml. An in vivo guinea pig bronchoconstriction (induced by LTD4) assay is also presented. Compound D gave ED50 (mg/kg) values of 1.0 and 0.0023 for po and iv administration respectively. LD50 values (mg/kg) were found to be < 300 and < 1000 for iv and po administration.
Chemistry: 2-[(E)-2-(3-(3-carboxy-3-ethylvalerylamino)phenyl)ethenyl[-6-[4-(ethyl phenyl)-butoxy]-methylpyridine (compound D) is one of thirty-five compounds specifically claimed. Preparative details using standard techniques are presented.
Structure: