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Englishfor 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., Plescia, F., Trincavelli, M., 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].
| Data di pubblicazione: | 2012 | |
| Titolo: | Synthesis, benzodiazepine receptor binding and molecular modelling of isochromeno[4,3-c]pyrazol-5(1H)-one derivatives | |
| Autori: | ||
| Citazione: | Maggio, B., Raffa, D., Raimondi, M., Plescia, F., Trincavelli, M., 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]. | |
| Rivista: | ||
| Digital Object Identifier (DOI): | http://dx.doi.org/ejmech.2012.06.028 | |
| 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. | |
| Settore Scientifico Disciplinare: | Settore CHIM/08 - Chimica Farmaceutica | |
| Appare nelle tipologie: | 1.01 Articolo in rivista |
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