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5-Lipoxygenase inhibition by N-hydroxycarbamates in dual-function compounds
Timothy A Lewis1, Lynn Bayless, Alan J DiPesa
1UCB Research, 840 Memorial Dr., Cambridge, MA 02139, USA. timlewis1201@comcast.net
Bioorganic & Medicinal Chemistry Letters
|February 3, 2005
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.