The synthesis of the (+)- and (-)-isomers of 3-methyl-5-carboxy-thyen-2-yl-glycine (3-MATIDA), heterocyle isosters of carboxyphenylglycines (CPGs), a known class of competitive metabotropic glutamate receptors, was accomplished by a stereoselective Ugi condensation. The two isomers were tested as potential rat mGluR1 ligand and the (+) isomer was found to be a moderately potent antagonist, while the (-) one was inactive.
Stereoselective Synthesis and Preliminary Evaluation of (+)- and (-)-3-methyl-5-carboxy-thien-2-yl-glycine (3-MATIDA): Identification of (+)-3-MATIDA as a Novel mGluR1 Competitive Antagonist
COSTANTINO, Gabriele;MARINOZZI, Maura;CAMAIONI, Emidio;NATALINI, Benedetto;PELLICCIARI, Roberto
2004
Abstract
The synthesis of the (+)- and (-)-isomers of 3-methyl-5-carboxy-thyen-2-yl-glycine (3-MATIDA), heterocyle isosters of carboxyphenylglycines (CPGs), a known class of competitive metabotropic glutamate receptors, was accomplished by a stereoselective Ugi condensation. The two isomers were tested as potential rat mGluR1 ligand and the (+) isomer was found to be a moderately potent antagonist, while the (-) one was inactive.File in questo prodotto:
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