Synthesis of a New Family of Surface Active Agents The Enkephalin Alkyl Amides

✍ Scribed by Reig, F. ;García Antón, J. M. ;Valencia, G. ;García Domínguez, J. J.

• Publisher: John Wiley and Sons
• Year: 1981
• Weight: 363 KB
• Volume: 83
• Category: Article
• ISSN: 0931-5985
• DOI: 10.1002/lipi.19810830910

✦ Synopsis

Abstract

Hydrophobic alkyl residues of different chain length have been covalently linked to the terminal carboxyl group of the enkephalin sequence, through the amide bond formation. The strategy of synthesis involves the preparation of the tetrapeptide: di‐Z‐Tyr‐Gly‐Gly‐Phe, by using the liquid phase method and N‐hydroxysuccinimide active ester as coupling agent, being this acylating group the one providing better yields. Such hydrophobic residues would enhance diffusion of enkephalins through lipidic structures, allowing, in some extent, the possibility of crossing the blood brain barrier, exhibiting as a consequence, long lasting analgetic effect.