Synthesis and evaluation of azalanstat analogues as heme oxygenase inhibitors

  • Bioorg Med Chem Lett. 2005 Mar 1;15(5):1457-61. doi: 10.1016/j.bmcl.2004.12.075.
Jason Z Vlahakis  1 ,  Robert T Kinobe ,  Raymond J Bowers ,  James F Brien ,  Kanji Nakatsu ,  Walter A Szarek
Affiliations
  • 1. Departments of Chemistry, Queen's University, Kingston, ON K7L 3N6, Canada.
PMID: 15713406 DOI: 10.1016/j.bmcl.2004.12.075
Abstract

Several analogues based on the lead structure of azalanstat were synthesized and evaluated as novel inhibitors of heme oxygenase (HO). A number of these compounds, which are structurally distinct from metalloporphyrin HO inhibitors, were found to be selective for the HO-1 isozyme (stress induced), and had substantially less inhibitory activity on HO-2, the constitutive isozyme.

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