Tricyclic Heteroaromatic Systems. Pyrazolo[3,4-c]quinolin-4-ones and Pyrazolo[3,4-c]quinoline-1,4-diones: Synthesis and Benzodiazepine Receptor Activity
β Scribed by Daniela Catarzi; Vittoria Colotta; Flavia Varano; Lucia Cecchi; Guido Filacchioni; Alessandro Galli; Chiara Costagli
- Publisher
- John Wiley and Sons
- Year
- 1997
- Tongue
- English
- Weight
- 393 KB
- Volume
- 330
- Category
- Article
- ISSN
- 0365-6233
No coin nor oath required. For personal study only.
β¦ Synopsis
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 optional proton acceptor at position-1, while the inactivity of the 1,4-dione derivatives 15-17 is due to the lack of the essential proton acceptor at position-3. These conclusions confirm the validity of our proposed pharmacophoric model.
I
π SIMILAR VOLUMES
## Abstract Some 1,2,4βtriazolo[4,3β__a__]quinoxalines 1β10, and 1,2,4βtriazino[4,3β__a__]quinoxalines 11β12 were prepared and biologically evaluated for their binding at the benzodiazepine receptor (BZR) in rat cortical membranes. The BZR affinity of 1β10 demonstrates that the presence of a proton
## Abstract Derivatives **7**β**13** of a new tricyclic heteroaromatic system, pyrido[3β²,2β²:5,6]thiopyrano[4,3β__c__]pyridazinβ3(2__H__,5__H__)βone, were prepared as potential ligands at the benzodiazepine receptor, in view of their structural analogy with potent ligands such as the pyrazoloquinoli