Consequences of cis-amide bond simulation in opioid peptides
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Six analogs of leucine-enkephalin were synthesized in which a 1,5-disubstituted tetrazole ring was incorporated in order to lock selected peptide bonds in cis geometry. The obtained compounds were examined based on their biological effects in vivo and in vitro. Only one analog was completely inactive in binding assays being very weakly active in the antinociceptive test. The remaining five compounds displayed at least weak receptor affinity and in vivo activity.
Key wordscis peptide bond conformation 1,5-disubstituted tetrazole ring Leu-enkephalin
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