Abstract
This report describes the evaluation of a wide range of structurally diverse “privileged structures”, either amines or acids, linked via urea and amide connections, to the key dipeptide D-Trp-Lys-OMe. This led to the discovery of a collection of potent and structurally distinct SSTR2 ligands in both the amide and urea series. The 4- (benzimidazolone)-piperidine linked SSTR2 agonist (8) is highlighted.
Keywords: peptidyl privileged structures, somatostatin receptor ligands, d-trp-lys-ome, (benzimidazolone)-piperidine
Letters in Drug Design & Discovery
Title: Diverse Peptidyl Privileged Structures as Potent Somatostatin Receptor Ligands
Volume: 1 Issue: 2
Author(s): Alexander Pasternak, Yanping Pan, Ralph T. Mosley, Susan P. Rohrer, Elizabeth T. Birzin, James Schaeffer, Arthur A. Patchett and Lihu Yang
Affiliation:
Keywords: peptidyl privileged structures, somatostatin receptor ligands, d-trp-lys-ome, (benzimidazolone)-piperidine
Abstract: This report describes the evaluation of a wide range of structurally diverse “privileged structures”, either amines or acids, linked via urea and amide connections, to the key dipeptide D-Trp-Lys-OMe. This led to the discovery of a collection of potent and structurally distinct SSTR2 ligands in both the amide and urea series. The 4- (benzimidazolone)-piperidine linked SSTR2 agonist (8) is highlighted.
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Cite this article as:
Pasternak Alexander, Pan Yanping, Mosley T. Ralph, Rohrer P. Susan, Birzin T. Elizabeth, Schaeffer James, Patchett A. Arthur and Yang Lihu, Diverse Peptidyl Privileged Structures as Potent Somatostatin Receptor Ligands, Letters in Drug Design & Discovery 2004; 1 (2) . https://dx.doi.org/10.2174/1570180043485563
DOI https://dx.doi.org/10.2174/1570180043485563 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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