Amino acids and peptides. XXXVI. Synthesis of enkephalin chloromethyl ketone and evaluation of its inhibitory activity against endopeptidase 22.19

Article abstract of DOI:10.1248/cpb.41.2038

Boc-Tyr-Gly-Gly-Phe-Leu-CH₂Cl was synthesized by the conventional solution method. During the course of acid hydrolysis (6N HCl, 110°C, 18h) of Boc-Phe-Leu-CH₂Cl, side reaction occurred, resulting in low recovery of Phe residue on amino acid analysis. The inhibitory activity of the synthesized Boc-Tyr-Gly-Gly-Phe-Leu-CH₂Cl against endopeptidase 22.19, an enzyme related to the metabolism of opioid peptides, was examined.

Full text of DOI:10.1248/cpb.41.2038

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