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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…

Index: Costantino, Gabriele; Marinozzi, Maura; Camaioni, Emidio; Natalini, Benedetto; Sarichelou, Iran; Micheli, Fabrizio; Cavanni, Paolo; Faedo, Stefania; Noe, Christian; Moroni, Flavio; Pellicciari, Roberto Farmaco, 2004 , vol. 59, # 2 p. 93 - 99

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Citation Number: 12

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.