SAR-study on a new class of imidazo[1,2-a]pyridine-based inhibitors of 5-lipoxygenase
2012
Hieke, Martina | Rödl, Carmen B. | Wisniewska, Joanna M. | la Buscató, Estel | Stark, Holger | Schubert-Zsilavecz, Manfred | Steinhilber, Dieter | Hofmann, Bettina | Proschak, Ewgenij
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 (IC₅₀=0.16μM (intact cells) and 0.1μM (cell-free)), which may possess potential as an effective lead compound intervening with inflammatory diseases and certain types of cancer.
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Эту запись предоставил National Agricultural Library