Stereoselective synthesis and preliminary evaluation of (+)-and (–)-3-methyl-5-carboxy-thien-2-yl-glycine (3-MATIDA): identification of (+)-3-MATIDA as a novel …
…, B Natalini, I Sarichelou, F Micheli, P Cavanni, S Faedo…
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.
