Novel AMPA and kainate receptor antagonists containing the pyrazolo[1,5-c]quinazoline ring system: synthesis and structure-activity relationships
In: Università degli studi di Firenze-IRIS
Online
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Zugriff:
This paper reports the synthesis and AMPA, Gly/NMDA, and KA receptor binding affinities of a new set of 1,9-disubstituted-8-chloro-pyrazolo[1,5- c ]quinazoline-2-carboxylates 2 – 34 . Binding data show that, in general, compounds 2 – 34 bind to the AMPA receptor with good affinity and selectivity. In particular, the obtained results indicate that the contemporary presence of a 1,2-dicarboxylic acid moiety and suitable benzo-substituents on the PQZ system is important to gain selective AMPA receptor antagonists. Moreover, this study shows that the presence of a 2-carboxybenzoylamino substituent at position-9 (compounds 33 – 34 ) is important for obtaining selective KA receptor antagonists. Some selected compounds were also tested for their functional antagonistic activity at both AMPA and NMDA receptor-ion channels.
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Novel AMPA and kainate receptor antagonists containing the pyrazolo[1,5-c]quinazoline ring system: synthesis and structure-activity relationships
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Autor/in / Beteiligte Person: | Lenzi, Ombretta ; Colotta, Vittoria ; Costagli, Chiara ; Galli, Alessandro ; Filacchioni, Guido ; Varano, Flavia ; Catarzi, Daniela |
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Quelle: | Università degli studi di Firenze-IRIS |
Medientyp: | unknown |
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