Decahydroisoquinoline derivatives as novel non-peptidic, potent and subtype-selective somatostatin sst3 receptor antagonists
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Troxler, Thomas J., Hurth, Konstanze, Schuh, Karl Heinrich, Schoeffter, Philippe, Langenegger, Daniel, Enz, Albert and Hoyer, Daniel (2010) Decahydroisoquinoline derivatives as novel non-peptidic, potent and subtype-selective somatostatin sst3 receptor antagonists. Bioorganic and Medicinal Chemistry Letters, 20 (5). pp. 1728-1734. ISSN 0960-894X
Abstract
Starting from non-peptidic sst1-selective somatostatin receptor antagonists, first compounds with mixed sst1/sst3 affinity were identified by directed structural modifications.Structural modifications on non-peptidic sst1-selective somatostatin receptor antagonists led to first derivatives with mixed sst1/sst3 affinity. 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 synthesized and show promising PK properties in rodents.
| Item Type: | Article |
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| Additional Information: | Author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used |
| Keywords: | Somatostatin; GPCR; Somatostatin sst3 receptor; Non-peptidic somatostatin receptor ligands; Subtype-selective sst3 receptor antagonists |
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| Date Deposited: | 13 Oct 2015 13:16 |
| Last Modified: | 13 Oct 2015 13:16 |
| URI: | https://oak.novartis.com/id/eprint/1966 |