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.
|Numero di pagine||12|
|Rivista||European Journal of Medicinal Chemistry|
|Stato di pubblicazione||Published - 2012|
All Science Journal Classification (ASJC) codes
- Drug Discovery
- Organic Chemistry
Maggio, B., Raffa, D., Plescia, F., Raimondi, M. V., Daidone, G., Basile, Trincavelli, Meneghetti, F., Guccione, & Martini (2012). Synthesis, benzodiazepine receptor binding and molecular modellingof isochromeno[4,3-c]pyrazol-5(1H)-one derivatives. European Journal of Medicinal Chemistry, 54, 709-720.