Journal
CHEMMEDCHEM
Volume 7, Issue 5, Pages 897-902Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201100602
Keywords
carbon monoxide; heme; heme oxygenases; imidazoles; inhibitors
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Funding
- Canadian Institutes of Health Research [MOP 64305]
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Several a-(1H-imidazol-1-yl)-?-phenylalkanes were synthesized and evaluated as novel inhibitors of heme oxygenase (HO). These compounds were found to be potent and selective for the stress-induced isozyme HO-1, showing mostly weak activity toward the constitutive isozyme HO-2. The introduction of an oxygen atom in the alkyl linker produced analogues with decreased potency toward HO-1, whereas the presence of a sulfur atom in the linker gave rise to analogues with greater potency toward HO-1 than the carbon-containing analogues. The most potent compounds studied contained a five-atom linker between the imidazolyl and phenyl moieties, whereas the most HO-1-selective compounds contained a four-atom linker between these groups. The compounds with a five-atom linker containing a heteroatom (O or S) were found to be the most potent inhibitors of HO-2; 1-(N-benzylamino)-3-(1H-imidazol-1-yl)propane dihydrochloride, with a nitrogen atom in the linker, was found to be inactive.
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