Comparative study of the affinity and metabolism of type I and type II binding quinoline carboxamide analogues by cytochrome P450 3A4

UP Dahal, C Joswig-Jones…

文献索引：Dahal, Upendra P.; Joswig-Jones, Carolyn; Jones, Jeffrey P. Journal of Medicinal Chemistry, 2012 , vol. 55, # 1 p. 280 - 290

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被引用次数: 16

摘要

Compounds that coordinate to the heme-iron of cytochrome P450 (CYP) enzymes are assumed to increase metabolic stability. However, recently we observed that the type II binding quinoline carboxamide (QCA) compounds were metabolically less stable. To test if the higher intrinsic clearance of type II binding compounds relative to type I binding compounds is general for other metabolic transformations, we synthesized a library of ...