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Synthetic routes to the neuropeptide Y Y1 receptor antagonist 1229U91 and related analogues for SAR studies and cell-based imaging

Abstract

The potent Y1 receptor antagonist, 1229U91 has an unusual cyclic dimer structure that makes syntheses of analogue series quite challenging. We have examined three new routes to the synthesis of such peptides that has given access to novel structural variants including heterodimeric compounds, ring size variants and labelled conjugates. These compounds, including a fluorescently labelled analogue VIII show potent antagonism that can be utilised in studying Y1 receptor pharmacology.

Type Journal
Authors Mountford, S.J.; Liu, M.; Zhang, L.; Groenen, M.; Herzog, H.; Holliday, N.; Thompson, P.E.
Publisher Name ORG BIOMOL CHEM
Published Date 2014-05-28 00:00:00
Published Volume 12
Published Issue 20
Published Pages 3271-81
URL http://www.ncbi.nlm.nih.gov/pubmed/24733083
Status Published in-print