Potholing of the hydrophobic heme oxygenase-1 western region for the search of potent and selective imidazole-based inhibitors.

@article{Salerno2018PotholingOT,
  title={Potholing of the hydrophobic heme oxygenase-1 western region for the search of potent and selective imidazole-based inhibitors.},
  author={L. Salerno and E. Amata and G. Romeo and A. Marrazzo and O. Prezzavento and Giuseppe Floresta and V. Sorrenti and I. Barbagallo and A. Rescifina and V. Pittal{\`a}},
  journal={European journal of medicinal chemistry},
  year={2018},
  volume={148},
  pages={
          54-62
        }
}
Here we report the design, synthesis, and molecular modeling of new potent and selective imidazole-based HO-1 inhibitors in which the imidazole nucleus and the hydrophobic groups are linked by a phenylethanolic spacer. Most of the tested compounds showed a good inhibitor activity with IC50 values in the low micromolar range, with two of them (1b and 1j) exhibiting also high selectivity toward HO-2. These results were obtained by the idea of potholing the entire volume of the principal… Expand
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