SAR-study on a new class of imidazo[1,2-a]pyridine-based inhibitors of 5-lipoxygenase.

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Hieke M, Rodl CB, Wisniewska JM, la Buscato E, Stark H, Schubert-Zsilavecz M, Steinhilber D, Hofmann B, Proschak E

SAR-study on a new class of imidazo[1,2-a]pyridine-based inhibitors of 5-lipoxygenase.

Bioorg Med Chem Lett. 2012 Mar 1;22(5):1969-75. doi: 10.1016/j.bmcl.2012.01.038. Epub 2012 Jan 24.

PubMed ID

22326163 [ View in PubMed

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Abstract

A novel class of 5-lipoxygenase (5-LO) inhibitors characterized by a central imidazo[1,2-a]pyridine scaffold, a cyclohexyl moiety and an aromatic system, is presented. This scaffold was identified in a virtual screening study and exhibits promising inhibitory potential on the 5-LO. Here, we investigate the structure-activity relationships of this compound class. With N-cyclohexyl-6-methyl-2-(4-morpholinophenyl)imidazo[1,2-a]pyridine-3-amine (14), we identified a potent 5-LO inhibitor (IC(50)=0.16muM (intact cells) and 0.1muM (cell-free)), which may possess potential as an effective lead compound intervening with inflammatory diseases and certain types of cancer.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Zileuton	Arachidonate 5-lipoxygenase	IC 50 (nM)	500	N/A	N/A	Details