Discovery of novel non-peptidic beta-alanine piperazine amide derivatives and their optimization to achiral, easily accessible, potent and selective somatostatin sst1 receptor antagonists.
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Troxler, Thomas J., Hurth, Konstanze, Mattes, Henri, Prashad, Mahavir, Schoeffter, Philippe, Langenegger, Daniel, Enz, Albert and Hoyer, Daniel (2009) Discovery of novel non-peptidic beta-alanine piperazine amide derivatives and their optimization to achiral, easily accessible, potent and selective somatostatin sst1 receptor antagonists. Bioorganic & Medicinal Chemistry Letters, 19 (5). pp. 1305-1309. ISSN 1464-3405
Abstract
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.
| 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 sst1 receptor; Selective sst1 receptor antagonists; Achiral; Non-peptidic somatostatin analogs |
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| Date Deposited: | 22 Feb 2010 11:50 |
| Last Modified: | 31 Jan 2013 00:50 |
| URI: | https://oak.novartis.com/id/eprint/1802 |