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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. Copyright © 2011 Elsevier Ltd. All rights reserved.


Frédéric J J Bihel, Hélène Justiniano, Martine Schmitt, Malik Hellal, Mohamed A Ibrahim, Claire Lugnier, Jean-Jacques Bourguignon. New PDE4 inhibitors based on pharmacophoric similarity between papaverine and tofisopam. Bioorganic & medicinal chemistry letters. 2011 Nov 1;21(21):6567-72

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PMID: 21920746

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