Application of the Guanidine–Acylguanidine Bioisosteric Approach to Argininamide??Type NPY Y2 Receptor Antagonists

…, R Ziemek, N Pop, G Bernhardt, A Buschauer

Index: Pluym, Nikola; Brennauer, Albert; Keller, Max; Ziemek, Ralf; Pop, Nathalie; Bernhardt, Guenther; Buschauer, Armin ChemMedChem, 2011 , vol. 6, # 9 p. 1727 - 1738

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Citation Number: 14

Abstract

Abstract Strongly basic groups such as guanidine moieties are crucial structural elements, but they compromise the drug-likeness of numerous biologically active compounds, including ligands of G-protein-coupled receptors (GPCRs). As part of a project focused on the search for guanidine bioisosteres, argininamide-type neuropeptide Y (NPY) Y 2 receptor (Y 2 R) antagonists related to BIIE0246 were synthesized. Starting from ornithine ...