Abstract
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.
Original language | English (US) |
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Pages (from-to) | 437-440 |
Number of pages | 4 |
Journal | International Journal of Peptide Research and Therapeutics |
Volume | 5 |
Issue number | 5-6 |
DOIs | |
State | Published - Jan 1 1998 |
Keywords
- 1,5-disubstituted tetrazole ring
- Cis peptide bond conformation
- Leu-enkephalin
ASJC Scopus subject areas
- Analytical Chemistry
- Bioengineering
- Biochemistry
- Molecular Medicine
- Drug Discovery