for their ability to displace specific [3H]flunitrazepam from bovine brain membranes. The substitution pattern of the above derivatives was shown to influence the receptor affinity. The most active compound of the series was 7e, showing a 54% inhibition of [3H]flunitrazepam binding. Compounds 7aed,i were compared with the known isomers chromeno[4,3-c]pyrazole-4(1H)-ones 14aed,i, showing that the isochromene/chromene isomerism influences the activity.
Maggio, B., Raffa, D., Raimondi, M.V., Plescia, F., Trincavelli, M.L., Martini, C., et al. (2012). Synthesis, benzodiazepine receptor binding and molecular modelling of isochromeno[4,3-c]pyrazol-5(1H)-one derivatives. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 54, 709-720 [ejmech.2012.06.028].
Synthesis, benzodiazepine receptor binding and molecular modelling of isochromeno[4,3-c]pyrazol-5(1H)-one derivatives
MAGGIO, Benedetta;RAFFA, Demetrio;RAIMONDI, Maria Valeria;PLESCIA, Fabiana;DAIDONE, Giuseppe
2012-01-01
Abstract
for their ability to displace specific [3H]flunitrazepam from bovine brain membranes. The substitution pattern of the above derivatives was shown to influence the receptor affinity. The most active compound of the series was 7e, showing a 54% inhibition of [3H]flunitrazepam binding. Compounds 7aed,i were compared with the known isomers chromeno[4,3-c]pyrazole-4(1H)-ones 14aed,i, showing that the isochromene/chromene isomerism influences the activity.
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