5-lipoxygenase inhibitors with histamine H(1) receptor antagonist activity.
Lewis TA, Bayless L, Eckman JB, Ellis JL, Grewal G, Libertine L, Marie Nicolas J, Scannell RT, Wels BF, Wenberg K, Wypij DM.
A series of novel compounds with both 5-lipoxygenase (5-LO) inhibitory and histamine H(1) receptor antagonist activity were designed for the treatment of asthma. These dual-function compounds were made by connecting 5-LO and H(1) pharmacophores,N-hydroxyureas and benzhydryl piperazines, respectively. A range of in vitro activities was observed, with the furan analog 10 demonstrating both activities in an animal model. The activities observed were compared to single-function drugs.