Synthesis and pharmacological characterisation of a conformationally restrained series of indole-2-carboxylates as in vivo potent glycine antagonists
โ Scribed by Romano Di Fabio; Gianluca Araldi; Davide Baraldi; Alfredo Cugola; Daniele Donati; Paola Gastaldi; Simone A Giacobbe; Fabrizio Micheli; Giorgio Pentassuglia
- Book ID
- 114018996
- Publisher
- Elsevier Science
- Year
- 2001
- Tongue
- English
- Weight
- 154 KB
- Volume
- 56
- Category
- Article
- ISSN
- 0014-827X
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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 o
Synthesis and Biological Evaluation of a Series of Quinazoline-2carboxylic Acids and Quinazoline-2,4-diones as Glycine-NMDA Antagonists: A Pharmacophore Model Based Approach. -Although the compounds studied contain all features required by the antagonist pharmacophore model, they only show poor aff