Kuhn, Kilian K., Ertl, Thomas, Dukorn, Stefanie, Keller, Max, Bernhardt, Günther, Reiser, Oliver and Buschauer, Armin
(2016)
High affinity agonists of the neuropeptide Y (NPY) Y4 receptor derived from the C-terminal pentapeptide of human pancreatic polypeptide (hPP): synthesis, stereochemical discrimination and radiolabeling.
Journal of Medicinal Chemistry 59 (13), pp. 6045-6058.
Full text not available from this repository.
Abstract
The diastereomeric mixture of D/L-2,7-diaminooctanedioyl-bis(YRLRY-NH2) (BVD-74D, 2) was described in the literature as a high affinity Y4 receptor agonist. Here we report on the synthesis and pharmacological characterization of the pure diastereomers (2R,7R)- and (2S,7S)-2 and a series of homo- and heterodimeric analogues in which octanedioic acid was used as an achiral linker. To investigate ...

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Item type: | Article | ||||||
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Date: | 25 May 2016 | ||||||
Additional Information (public): | Supplementary material available | ||||||
Institutions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Oliver Reiser | ||||||
Projects: | GRK 1910, Graduiertenkolleg "Medicinal Chemistry of Selective GPCR Ligands" | ||||||
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Keywords: | Bioisosteric replacement, carbamoylguanidine, cross-metathesis, diastereomers, neuropeptide Y, NPY Y4 receptor agonist, pancreatic polypeptide, radioligand | ||||||
Dewey Decimal Classification: | 500 Science > 540 Chemistry & allied sciences 600 Technology > 615 Pharmacy | ||||||
Status: | Published | ||||||
Refereed: | Yes, this version has been refereed | ||||||
Created at the University of Regensburg: | Yes | ||||||
Item ID: | 33565 |