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Isozyme-Selective Heme Oxygenase Inhibitors:Design,Synthesis,and Biological Evaluation

Jason Z.VlahakisRobert T.KinobeGheorghe RomanJames F.BrienKanji NakatsuWalter A.Szarek

Departments of Chemistry Queen’s University,Kingston,Ontario,Canada K7L 3N6Pharmacology & Toxicology Queen’s University,Kingston,Ontario,Canada K7L 3N6

摘要:<正> Several imidazole-containing compounds were synthesized and evaluated as novel inhibitors of heme oxygenase (HO). A number of these compounds showed enhanced activity for HO over other heme - dependent enzymes (such as NOS and sGC).In addition, some of these compounds were highly selective for the inhibition of HO-1(inducible isozyme) compared with HO - 2 (constitutive isozyme). One of the compounds.QC-13,exhibits an IC50 value of 0.8±0.2 mM for HO - 1 (rat spleen) and approximately 305 mM for HO - 2 (rat brain). Over 100 compounds have been synthesized, and structure activity relationships amongst these analogues with respect to the inhibition of HO and other enzymes will be presented. These drugs are anticipated to become useful tools in elucidating the physiological/pathological roles of HO/carbon monoxide in mammalian and other biological systems.
会议名称:

第十五届国际药理学大会

会议时间:

2006-07

会议地点:

中国北京

  • 专辑:

    医药卫生科技

  • 专题:

    基础医学

  • 分类号:

    R341

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