- New PDE4 inhibitors based on pharmacophoric similarity between papaverine and tofisopam.
New PDE4 inhibitors based on pharmacophoric similarity between papaverine and tofisopam.
Bioorganic & medicinal chemistry letters (2011-09-17)
Frédéric J J Bihel, Hélène Justiniano, Martine Schmitt, Malik Hellal, Mohamed A Ibrahim, Claire Lugnier, Jean-Jacques Bourguignon
PMID21920746
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.