title: 5-lipoxygenase inhibitors with histamine H(1) receptor antagonist activity.
abstract: 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.
authors.affiliation: UCB Research, 840 Memorial Dr, Cambridge MA 02139, USA. timothy.lewis@ucb-group.com
authors.forename: Timothy A
authors.initials: TA
authors.lastname: Lewis
authors.forename: Lynn
authors.initials: L
authors.lastname: Bayless
authors.forename: Joseph B
authors.initials: JB
authors.lastname: Eckman
authors.forename: James L
authors.initials: JL
authors.lastname: Ellis
authors.forename: Gurmit
authors.initials: G
authors.lastname: Grewal
authors.forename: Lyn
authors.initials: L
authors.lastname: Libertine
authors.forename: Jean
authors.initials: J
authors.lastname: Marie Nicolas
authors.forename: Ralph T
authors.initials: RT
authors.lastname: Scannell
authors.forename: Bruce F
authors.initials: BF
authors.lastname: Wels
authors.forename: Karen
authors.initials: K
authors.lastname: Wenberg
authors.forename: Donna M
authors.initials: DM
authors.lastname: Wypij
mesh_terms: D000818:Animals; D018938:Caco-2 Cells; D006634:Histamine H1 Antagonists / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D006801:Humans; D016859:Lipoxygenase Inhibitors / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D008862:Microsomes, Liver / Q000378:metabolism; D051381:Rats
chemical_list: D006634:Histamine H1 Antagonists; D016859:Lipoxygenase Inhibitors