title: 5-Lipoxygenase inhibition by N-hydroxycarbamates in dual-function compounds.
abstract: A series of N-hydroxycarbamates containing a histaminergic H(1) receptor antagonist pharmacophore was synthesized. In vitro assays determined the compounds had both histaminergic binding and 5-lipoxygenase inhibiting activities comparable to the corresponding N-hydroxyurea analog. Animal models demonstrated antihistaminergic and the 5-lipopxygenase inhibitory activity, with the N-hydroxyurea analog having a better overall profile.
authors.affiliation: UCB Research, 840 Memorial Dr., Cambridge, MA 02139, USA. timlewis1201@comcast.net
authors.forename: Timothy A
authors.initials: TA
authors.lastname: Lewis
authors.forename: Lynn
authors.initials: L
authors.lastname: Bayless
authors.forename: Alan J
authors.initials: AJ
authors.lastname: DiPesa
authors.forename: Joseph B
authors.initials: JB
authors.lastname: Eckman
authors.forename: Michel
authors.initials: M
authors.lastname: Gillard
authors.forename: Lyn
authors.initials: L
authors.lastname: Libertine
authors.forename: Ralph T
authors.initials: RT
authors.lastname: Scannell
authors.forename: Donna M
authors.initials: DM
authors.lastname: Wypij
authors.forename: Michelle A
authors.initials: MA
authors.lastname: Young
mesh_terms: D000818:Animals; D001769:Blood; D006168:Guinea Pigs; D006634:Histamine H1 Antagonists / Q000138:chemical synthesis / Q000737:chemistry; D006801:Humans; D006877:Hydroxamic Acids / Q000138:chemical synthesis* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D007975:Leukotriene B4 / Q000096:biosynthesis; D016859:Lipoxygenase Inhibitors; D011485:Protein Binding; D013329:Structure-Activity Relationship
chemical_list: D006634:Histamine H1 Antagonists; D006877:Hydroxamic Acids; D016859:Lipoxygenase Inhibitors; D007975:Leukotriene B4