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Synthesis and Biological Evaluation of a Series of Quinazoline-2-carboxylic Acids and Quinazoline-2,4-diones as Glycine-NMDA Antagonists: A Pharmacophore Model Based Approach

✍ Scribed by Vittoria Colotta; Daniela Catarzi; Flavia Varano; Lucia Cecchi; Guido Filacchioni; Alessandro Galli; Chiara Costagli

Publisher: John Wiley and Sons
Year: 1997
Tongue: English
Weight: 500 KB
Volume: 330
Category: Article
ISSN: 0365-6233
DOI: 10.1002/ardp.19973300504

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✦ Synopsis

The synthesis and glycine-NMDA binding activity of a series of quinazoline-2-carboxylic acids 1 and quinazoline-2,4-diones 2, containing all the essential and optional pharmacophoric descriptors required by a putative glycine antagonist model, are reported. The binding results show that only three of the title compounds displayed micromolar receptor affinity, demonstrating how disappointing the synthesis of receptor ligands based only on interaction models can be.

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