Decahydroisoquinoline derivatives as novel non-peptidic, potent and subtype-selective somatostatin sst 3 receptor antagonists

…, KH Schuh, P Schoeffter, D Langenegger, A Enz…

文献索引：Troxler, Thomas; Hurth, Konstanze; Schuh, Karl-Heinrich; Schoeffter, Philippe; Langenegger, Daniel; Enz, Albert; Hoyer, Daniel Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 5 p. 1728 - 1734

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被引用次数: 12

摘要

Starting from non-peptidic sst1-selective somatostatin receptor antagonists, first compounds with mixed sst1/sst3 affinity were identified by directed structural modifications. Systematic optimization of these initial leads afforded novel, enantiomerically pure, highly potent and sst3-subtype selective somatostatin antagonists based on a (4S, 4aS, 8aR)- decahydroisoquinoline-4-carboxylic acid core moiety. These compounds can efficiently be ...