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Decahydroisoquinoline derivatives as novel non-peptidic, potent and subtype-selective somatostatin sst3 receptor antagonists

Troxler, Thomas J. and Hurth, Konstanze and Schuh, Karl Heinrich and Schoeffter, Philippe and Langenegger, Daniel and 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

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