New PDE4 inhibitors based on pharmacophoric similarity between papaverine and tofisopam

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 derivative...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-11, Vol.21 (21), p.6567-6572
Hauptverfasser:	Bihel, Frédéric J.J., Justiniano, Hélène, Schmitt, Martine, Hellal, Malik, Ibrahim, Mohamed A., Lugnier, Claire, Bourguignon, Jean-Jacques
Format:	Artikel
Sprache:	eng
Schlagworte:	Benzodiazepine benzodiazepines Benzodiazepines - chemistry Benzodiazepines - pharmacology Benzophenone Biochemistry, Molecular Biology Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Cellular Biology chemical derivatives enzyme inhibitors Inhibitory Concentration 50 Life Sciences Medical sciences papaverine Papaverine - chemistry Papaverine - pharmacology Pharmacology. Drug treatments Phosphodiesterase Phosphodiesterase 4 Inhibitors - chemistry Phosphodiesterase 4 Inhibitors - pharmacology phosphoric diester hydrolases Respiratory system
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2011.08.036