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Valeria Sorrenti, Salvatore Guccione, Claudia Di Giacomo, Maria N. Modica, Valeria Pittalà, Rosaria Acquaviva, Livia Basile, Morena Pappalardo and Loredana Salerno Evaluation of Imidazole-Based Compounds as Heme Oxygenase-1 Inhibitors Chemical Biology & Drug Design 80

Article first published online: 9 OCT 2012 | DOI: 10.1111/cbdd.12015

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Imidazole-based compounds were evaluated as inhibitors of heme oxygenase-1 (HO-1); most of tested compounds were good inhibitors with IC50 values in the low micromolar range. The binding of the most active compound 11 with heme-conjugated hHO-1 was also examined by spectral analyses; compound 11 was able to form a heme-compound 11 complex at low micromolar concentrations. Docking studies and pharmacophore analysis were performed to obtain informations on the binding mode; results were in agreement with experimental inhibition data.

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