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Application of the guanidine – acylguanidine bioisosteric approach to argininamide-type NPY Y2 receptor antagonists

Pluym, Nikola ; Brennauer, Albert ; Keller, Max ; Ziemek, Ralf ; Pop, Nathalie ; Bernhardt, Günther ; Buschauer, Armin



Abstract

Strongly basic groups such as guanidine moieties are crucial structural elements but compromising drug-likeness of numerous biologically active compounds including ligands of G-protein coupled receptors (GPCRs). As part of a project focusing on the search for guanidine bioisosteres, argininamide-type neuropeptide Y (NPY) Y2 receptor (Y2R) antagonists related to BIIE0246 were synthesized. Starting ...

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