Discovery of novel non-peptidic β-alanine piperazine amide derivatives and their optimization to achiral, easily accessible, potent and selective somatostatin sst 1 …

…, P Schoeffter, D Langenegger, A Enz, D Hoyer

Index: Troxler, Thomas; Hurth, Konstanze; Mattes, Henri; Prashad, Mahavir; Schoeffter, Philippe; Langenegger, Daniel; Enz, Albert; Hoyer, Daniel Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 5 p. 1305 - 1309

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Citation Number: 9

Abstract

Structural simplification of the core moieties of obeline and ergoline somatostatin sst1 receptor antagonists, followed by systematic optimization, led to the identification of novel, highly potent and selective sst1 receptor antagonists. These achiral, non-peptidic compounds are easily prepared and show promising PK properties in rodents.