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Synthesis, Enzymic Degradation, Lipophilic Properties, and Biological Activity of [D-Alanine2, t-butylglycine5]enkephalin Amide

✍ Scribed by Jean-Lue Fauchère; Claudia Petermann

Book ID: 102858478
Publisher: John Wiley and Sons
Year: 1980
Tongue: German
Weight: 508 KB
Volume: 63
Category: Article
ISSN: 0018-019X
DOI: 10.1002/hlca.19800630410

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✦ Synopsis

Abstract

L‐C^α^‐t‐Butylglycine (Bug), its amide, methyl ester, and N^α^‐t‐butoxycarbonyl derivative were prepared by an asymmetric synthesis, and the Hansch side‐chain hydrophobic (lipophilicity) parameter determined. A new enkephalin analogue, H · Tyr‐D‐Ala‐Gly‐Phe‐Bug · NH~2~ was synthesized which is pharmacologically active in two in vitro assays and strongly resistant against a number of enzymes in vitro.

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