New PDE4 inhibitors based on pharmacophoric similarity between papaverine and tofisopam

…, H Justiniano, M Schmitt, M Hellal, MA Ibrahim…

Index: Bihel, Frederic J.J.; Justiniano, Helene; Schmitt, Martine; Hellal, Malik; Ibrahim, Mohamed A.; Lugnier, Claire; Bourguignon, Jean-Jacques Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 21 p. 6567 - 6572

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Citation Number: 4

Abstract

Pharmacophoric comparison between papaverine and tofisopam led to identify three new series of micro-to sub-micromolar inhibitors of phosphodiesterase-4, including 7, 8-dialkoxy- 2, 3-benzodiazepin-4-one derivatives, 7, 8-dialkoxy-1, 4-benzodiazepin-2-one derivatives, and dialkoxybenzophenone derivatives.