The synthesis and Gly/NMDA, AMPA and KA receptor binding activities of some 3-hydroxy-quinazoline-2,4-dione derivatives are reported. The binding data, together with functional antagonism studies, showed that the 3-hydroxy-quinazoline-2,4- dione moiety can be considered a useful scaffold to obtain selective Gly/NMDA and AMPA receptor antagonists. In fact, introduction of chlorine atom(s) on precise position(s) of the benzofused moiety yielded Gly/NMDA selective antagonists, while the presence of the 6-(1,2,4-triazol-4-yl) group shifted the affinity and selectivity towards the AMPA receptor.

“3-Hydroxy-quinazoline-2,4-dione as a useful scaffold to obtain selective Gly/NMDA and AMPA receptor antagonists” / V. COLOTTA; D. CATARZI; F. VARANO; F. R. CALABRI; G. FILACCHIONI; C. COSTAGLI; A. GALLI.. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - STAMPA. - 14:(2004), pp. 2345-2349.

“3-Hydroxy-quinazoline-2,4-dione as a useful scaffold to obtain selective Gly/NMDA and AMPA receptor antagonists”

COLOTTA, VITTORIA;CATARZI, DANIELA;VARANO, FLAVIA;FILACCHIONI, GUIDO;C. COSTAGLI;A. GALLI
2004

Abstract

The synthesis and Gly/NMDA, AMPA and KA receptor binding activities of some 3-hydroxy-quinazoline-2,4-dione derivatives are reported. The binding data, together with functional antagonism studies, showed that the 3-hydroxy-quinazoline-2,4- dione moiety can be considered a useful scaffold to obtain selective Gly/NMDA and AMPA receptor antagonists. In fact, introduction of chlorine atom(s) on precise position(s) of the benzofused moiety yielded Gly/NMDA selective antagonists, while the presence of the 6-(1,2,4-triazol-4-yl) group shifted the affinity and selectivity towards the AMPA receptor.
2004
14
2345
2349
V. COLOTTA; D. CATARZI; F. VARANO; F. R. CALABRI; G. FILACCHIONI; C. COSTAGLI; A. GALLI.
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/208568
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