Acrylamide Derivatives as Antiallergic Agents.III. : Synthesis and Structure-Activity Relationships of N-[4-(4-Diphenylmethyl-1-piperazinyl)butyl]- and N-[4-(4-Diphenylmethylene-1-piperidyl)butyl]-3-heteroarylacrylamides

Abstract

A new series of 3-heteroarylacrylamides 2 and 4 was prepared and the inhibitory activities against the rat passive cutaneous anaphylaxis (PCA) reaction and the enzyme 5-lipoxygenase (5-LO) were tested. Most of the compounds exhibited an anti-PCA activity superior to or equivalent to ketotifen and had a 5-LO inhibitory activity. The 3-heteroarylacrylamide derivatives including 3-(3-pyridyl)acrylamides represent a new structural class of compound that exhibits not only an in vivo anti-PCA activity but also an in vitro 5-LO ingibitory activity.