SAR-study on a new class of imidazo[1,2-a]pyridine-based inhibitors of 5-lipoxygenase |
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Authors: | Hieke Martina Rödl Carmen B Wisniewska Joanna M la Buscató Estel Stark Holger Schubert-Zsilavecz Manfred Steinhilber Dieter Hofmann Bettina Proschak Ewgenij |
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Affiliation: | Institute of Pharmaceutical Chemistry, ZAFES/LiFF/OSF Goethe-University Frankfurt, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany. |
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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)=0.16μM (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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