Consequences of Cis-amide Bond Simulationin Opioid Peptides
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文摘
Six analogs of leucine-enkephalin were synthesized inwhich a 1,5-disubstituted tetrazole ring wasincorporated in order to lock selected peptide bondsin cis geometry. The obtained compounds wereexamined based on their biological effects in vivo andin vitro. Only one analog was completelyinactive in binding assays being very weakly active inthe antinociceptive test. The remaining five compoundsdisplayed at least weak receptor affinity and in vivo activity.