Tricyclic heteroaromatic systems: [1]Benzopyrano-pyrazol-4-ones as benzodiazepine receptor ligands
โ Scribed by Vittoria Colotta; Lucia Cecchi; Fabrizio Melani; Guido Filacchioni; Claudia Martini; Sabrina Gelli; Antonio Lucacchini
- Book ID
- 102408172
- Publisher
- John Wiley and Sons
- Year
- 1991
- Tongue
- English
- Weight
- 466 KB
- Volume
- 80
- Category
- Article
- ISSN
- 0022-3549
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โฆ Synopsis
The synthesis of a series of 8-substituted 1,4-dihydro-1-aryl-3-methyl-[1]benzopyrano[3,4-d]pyrazol-4-ones (series 7) 2,4-dihydro-2-aryl-3-methyl[1]benzopyrano[4,3-c]pyrazol-4-ones (series 8) is reported. Compounds of series 7 and 8 were tested for their ability to displace [3H]flunitrazepam from bovine brain membranes and for their in vitro biological activity. The results allowed some conclusions to be drawn about the structural requirements of the benzodiazepine recognition site within this class of unusual ligands.
๐ SIMILAR VOLUMES
Some pyrazolo[3,4-c~quinoline-4-ones 1-14 and pyrazolo[3.4-c]quinoline-I ,4-diones 15-17 were prepared and biologically evaluated for their binding at the benzodiazepine receptor (BZR) in rat cortical membranes. The moderate binding activity of 1-5,7,9-10, 13 is attributable to the lack of the optio