Studies with Inhibitors of Leukotriene Biosynthesis with Special Reference to Piriprost (U-60,257)

Abstract

The underlying and motivating force behind the search for inhibitors of the formation of the leukotrienes is the hypothesis that these substances play an important if not an etiologic role in the elicitation of the symptoms of inflammation in general and of asthma in particular. An essential element in the final “proof” of this assumption is the demonstration that the selective inhibition of the formation or action of these substances can result in meaningful improvement in the condition of patients suffering from these disorders. Thus, even though relatively non-selective inhibitors may have their place, and even though in certain circumstances it may actually be desirable to combine the specific inhibition of certain pathways in one and the same molecule, the goal of the studies to be reported here is the development of selective inhibitors of the formation of the leukotrienes in the hope that these agents might then be useful in providing the remaining needed element of proof for the role of the leukotrienes in disease.