5-Lipoxygenase inhibition by N-hydroxycarbamates in dual-function compounds.

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Lewis TA, Bayless L, DiPesa AJ, Eckman JB, Gillard M, Libertine L, Scannell RT, Wypij DM, Young MA

5-Lipoxygenase inhibition by N-hydroxycarbamates in dual-function compounds.

Bioorg Med Chem Lett. 2005 Feb 15;15(4):1083-5.

PubMed ID

15686917 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Cetirizine	Histamine H1 receptor	Ki (nM)	5.89	N/A	N/A	Details
Zileuton	Arachidonate 5-lipoxygenase	IC 50 (nM)	873	N/A	N/A	Details
Zileuton	Arachidonate 5-lipoxygenase	IC 50 (nM)	518	N/A	N/A	Details