N-(Pyridin-3-yl) benzamides as selective inhibitors of human aldosterone synthase (CYP11B2)

…, M Hafner, M Zender, D Ammann, RW Hartmann…

文献索引：Zimmer, Christina; Hafner, Marieke; Zender, Michael; Ammann, Dominic; Hartmann, Rolf W.; Vock, Carsten A. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 1 p. 186 - 190

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被引用次数: 16

摘要

A series of 23 N-(Pyridin-3-yl) benzamides was synthesized and evaluated for their potential to inhibit human steroid-11β-hydroxylase (CYP11B1) and human aldosterone synthase (CYP11B2). The most potent and selective CYP11B2 inhibitors (IC50 values 53–166nM) were further evaluated for their potential to inhibit human CYP17 and CYP19, and no inhibition was observed. Clear evidence was shown for N-(Pyridin-3-yl) benzamides to be ...