Synthesis, benzodiazepine receptor binding and molecular modellingof isochromeno[4,3-c]pyrazol-5(1H)-one derivatives

Benedetta Maggio, Demetrio Raffa, Maria Valeria Raimondi, Giuseppe Daidone, Fabiana Plescia, Basile, Trincavelli, Fiorella Meneghetti, Guccione, Martini

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for their ability to displace specific [3H]flunitrazepam from bovine brain membranes. The substitutionpattern of the above derivatives was shown to influence the receptor affinity. The most active compoundof the series was 7e, showing a 54% inhibition of [3H]flunitrazepam binding. Compounds 7aed,i werecompared with the known isomers chromeno[4,3-c]pyrazole-4(1H)-ones 14aed,i, showing that theisochromene/chromene isomerism influences the activity.
Original languageEnglish
Pages (from-to)709-720
Number of pages12
JournalEuropean Journal of Medicinal Chemistry
Publication statusPublished - 2012


All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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