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Synthesis and Opioid Activity of Tyr(1)–ψ[(Z)CF=CH]–Gly(2) and Tyr(1)–ψ[(S)/(R)-CF(3)CH–NH]–Gly(2) Leu-enkephalin Fluorinated Peptidomimetics

We describe the design, synthesis, and opioid activity of fluoroalkene (Tyr(1)–ψ[(Z)CF=CH]–Gly(2)) and trifluoroethylamine (Tyr(1)–ψ[(S)/(R)-CF(3)CH–NH]–Gly(2)) analogues of the endogenous opioid neuropeptide, Leu-enkephalin. The fluoroalkene peptidomimetic exihibited low nanomolar functional activi...

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Publicat a:ChemMedChem
Autors principals: Karad, Somnath Narayan, Pal, Mohan, Crowley, Rachel S., Prisinzano, Thomas E., Altman, Ryan A.
Format: Artigo
Idioma:Inglês
Publicat: 2017
Matèries:
Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC5486982/
https://ncbi.nlm.nih.gov/pubmed/28296145
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1002/cmdc.201700103
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