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Tricyclic Heteroaromatic Systems. Pyrazolo[3,4-c]quinolin-4-ones and Pyrazolo[3,4-c]quinoline-1,4-diones: Synthesis and Benzodiazepine Receptor Activity

✍ 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

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✦ 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.

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Tricyclic Heteroaromatic Systems. 1,2,4-
✍ Vittoria Colotta; Daniela Catarzi; Flavia Varano; Lucia Cecchi; Guido Filacchion πŸ“‚ Article πŸ“… 1997 πŸ› John Wiley and Sons 🌐 English βš– 416 KB

## Abstract Some 1,2,4‐triazolo[4,3‐__a__]quinoxalines 1–10, and 1,2,4‐triazino[4,3‐__a__]quinoxalines 11–12 were prepared and biologically evaluated for their binding at the benzodiazepine receptor (BZR) in rat cortical membranes. The BZR affinity of 1–10 demonstrates that the presence of a proton

Synthesis and Benzodiazepine Receptor Af
✍ Giampaolo Primofiore; Federico Da Settimo; Anna Maria Marini; Francesca Simorini πŸ“‚ Article πŸ“… 2005 πŸ› John Wiley and Sons 🌐 English βš– 125 KB πŸ‘ 1 views

## Abstract Derivatives **7**–**13** of a new tricyclic heteroaromatic system, pyrido[3β€²,2β€²:5,6]thiopyrano[4,3‐__c__]pyridazin‐3(2__H__,5__H__)‐one, were prepared as potential ligands at the benzodiazepine receptor, in view of their structural analogy with potent ligands such as the pyrazoloquinoli