5-lipoxygenase inhibitors with histamine H(1) receptor antagonist activity.
Article Details
- CitationCopy to clipboard
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]
- 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