5-lipoxygenase inhibitors with histamine H(1) receptor antagonist activity |
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| Authors: | Lewis Timothy A Bayless Lynn Eckman Joseph B Ellis James L Grewal Gurmit Libertine Lyn Marie Nicolas Jean Scannell Ralph T Wels Bruce F Wenberg Karen Wypij Donna M |
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| Institution: | UCB Research, 840 Memorial Dr, Cambridge MA 02139, USA. timothy.lewis@ucb-group.com |
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| 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. |
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