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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
Author(s) -
Colotta Vittoria,
Catarzi Daniela,
Varano Flavia,
Cecchi Lucia,
Filacchioni Guido,
Galli Alessandro,
Costagli Chiara
Publication year - 1997
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19973300504
Subject(s) - pharmacophore , chemistry , quinazoline , nmda receptor , glycine , stereochemistry , chemical synthesis , carboxylic acid , combinatorial chemistry , glycine receptor , antagonist , biological activity , carboxamide , receptor , amino acid , biochemistry , in vitro
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.