title: Synthesis and evaluation of azalanstat analogues as heme oxygenase inhibitors.
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.
authors.affiliation: Departments of Chemistry, Queen's University, Kingston, ON K7L 3N6, Canada.
authors.forename: Jason Z
authors.initials: JZ
authors.lastname: Vlahakis
authors.forename: Robert T
authors.initials: RT
authors.lastname: Kinobe
authors.forename: Raymond J
authors.initials: RJ
authors.lastname: Bowers
authors.forename: James F
authors.initials: JF
authors.lastname: Brien
authors.forename: Kanji
authors.initials: K
authors.lastname: Nakatsu
authors.forename: Walter A
authors.initials: WA
authors.lastname: Szarek
mesh_terms: D000814:Aniline Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006419:Heme Oxygenase (Decyclizing) / Q000037:antagonists & inhibitors*; D051547:Heme Oxygenase-1; D008968:Molecular Conformation; D051381:Rats; D013329:Structure-Activity Relationship; D013440:Sulfides / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D000814:Aniline Compounds; D004791:Enzyme Inhibitors; D013440:Sulfides; C082410:azalanstat; D006419:Heme Oxygenase (Decyclizing); D051547:Heme Oxygenase-1; C105245:heme oxygenase-2