5-lipoxygenase inhibitors with histamine H(1) receptor antagonist activity.

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Lewis TA, Bayless L, Eckman JB, Ellis JL, Grewal G, Libertine L, Marie Nicolas J, Scannell RT, Wels BF, Wenberg K, Wypij DM

5-lipoxygenase inhibitors with histamine H(1) receptor antagonist activity.

Bioorg Med Chem Lett. 2004 May 3;14(9):2265-8.

PubMed ID

15081022 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Cetirizine	Histamine H1 receptor	Ki (nM)	14	N/A	N/A	Details
Zileuton	Arachidonate 5-lipoxygenase	IC 50 (nM)	873	N/A	N/A	Details