| 19208473 |
Troxler T, Hurth K, Mattes H, Prashad M, Schoeffter P, Langenegger D, Enz A, Hoyer D: Discovery of novel non-peptidic beta-alanine piperazine amide derivatives and their optimization to achiral, easily accessible, potent and selective somatostatin sst1 receptor antagonists. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1305-9. Epub 2009 Jan 27.
Structural simplification of the core moieties of obeline and ergoline somatostatin sst (1) receptor antagonists, followed by systematic optimization, led to the identification of novel, highly potent and selective sst (1) receptor antagonists. These achiral, non-peptidic compounds are easily prepared and show promising PK properties in rodents. |
82(1,1,1,2) |