Abstract

Proline chimeras are conformationally rigid amino acid analogues. Their application in medicinal chemistry for the synthesis of peptidomimetics is a well-known approach. Of particular interest are the natural Glu/Asp proline chimeras, namely Domoic acid and Kainic acid, for their toxic effect on the human health which have been used as probes for glutamatergic receptors studies. In this review, we analyze the most relevant synthetic approaches to Glu/Asp analogues.

Keywords: Aspartic acid, domoic acid, glutamic acid, kainic acid, peptidomimetics, proline chimeras.

Graphical Abstract