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Consequences of Cis-amide Bond Simulation in Opioid Peptides |
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| Authors: | Jacek Olczak Krzysztof Kaczmarek Iwona Maszczyńska Marek Lisowski Dagmar Stropova Victor J Hruby Henry I Yamamura Andrzej W Lipkowski Janusz Zabrocki |
| Institution: | (1) Institute of Organic Chemistry, Technical University of łódź, Zwirki Str. 36, PL-90-924 łódź, Poland;(2) Medical Research Centre, Polish Academy of Sciences, PL-00-784 Warsaw, Poland;(3) Institute of Chemistry, University of Wrocław, PL-50-383 Wrocław, Poland;(4) Department of Pharmacology, University of Arizona, 85721 Tucson, AZ, U.S.A.;(5) Department of Chemistry, University of Arizona, 85721 Tucson, AZ, U.S.A. |
| Abstract: | Summary 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. |
| Keywords: | cis peptide bond conformation 1 5-disubstituted tetrazole ring Leu-enkephalin |
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