Novel AMPA and kainate receptor antagonists containing the pyrazolo[1,5-c]quinazoline ring system: Synthesis and structure-activity relationships.
In: Bioorganic & medicinal chemistry, Jg. 16 (2008-03-01), Heft 5, S. 2617-26
academicJournal
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.
Titel: |
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: | Varano, F ; Catarzi, D ; Colotta, V ; Lenzi, O ; Filacchioni, G ; Galli, A ; Costagli, C |
Zeitschrift: | Bioorganic & medicinal chemistry, Jg. 16 (2008-03-01), Heft 5, S. 2617-26 |
Veröffentlichung: | Oxford : Elsevier Science ; <i>Original Publication</i>: Oxford : New York : Pergamon Press, c1993-, 2008 |
Medientyp: | academicJournal |
ISSN: | 1464-3391 (electronic) |
DOI: | 10.1016/j.bmc.2007.11.046 |
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