Opioid activity of 4-imidazolidinone positional analogues of Leu-Enkephalin
| Autor: | Adel Nefzi, Markéta Rinnová, Richard A. Houghten |
|---|---|
| Rok vydání: | 2002 |
| Předmět: |
Magnetic Resonance Spectroscopy
Imidazolidinone Stereochemistry Clinical Biochemistry Receptors Opioid mu Pharmaceutical Science Sequence (biology) Methylene bridge Methylation Biochemistry Structure-Activity Relationship chemistry.chemical_compound Receptors Opioid delta Drug Discovery Moiety Receptor Molecular Biology Protein secondary structure Peptide sequence Chromatography High Pressure Liquid Receptors Opioid kappa Organic Chemistry Imidazoles Leu-enkephalin Analgesics Opioid chemistry Drug Design Molecular Medicine Indicators and Reagents Enkephalin Leucine |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 12:3175-3178 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(02)00678-9 |
| Popis: | Modulation of opioid activity was accomplished for analogues of Leu-enkephalin through incorporation of a 4-imidazolidinone moiety. The peptide backbone was constrained via a methylene bridge between two neighboring amides within its regular peptide sequence, which was expected to disrupt the secondary structure of the original molecule. Five positional analogues of Leu-enkephalin based on the same sequence and different location of the imidazolidinone-constrict were designed, synthesized, and examined for their affinity to micro-, delta- and kappa-opioid receptors. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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