SAR of the arylpiperazine moiety of obeline somatostatin sst sub(1) receptor antagonists

The SAR of over 50 derivatives of octahydrobenzo[g]quinoline (obeline)-type somatostatin sst sub(1) receptor antagonist 1 is presented, focusing on the modification of its arylpiperazine moiety. Sst sub(1) affinities in this series cover a range of five orders of magnitude with the best derivatives...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2007-07, Vol.17 (14), p.3988-3991
Main Authors: Hurth, Konstanze, Enz, Albert, Floersheim, Philipp, Gentsch, Conrad, Hoyer, Daniel, Langenegger, Daniel, Neumann, Peter, Pfaeffli, Paul, Sorg, Dieter, Swoboda, Robert, Vassout, Annick, Troxler, Thomas
Format: Article
Language:English
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Summary:The SAR of over 50 derivatives of octahydrobenzo[g]quinoline (obeline)-type somatostatin sst sub(1) receptor antagonist 1 is presented, focusing on the modification of its arylpiperazine moiety. Sst sub(1) affinities in this series cover a range of five orders of magnitude with the best derivatives displaying subnanomolar sst sub(1) affinities and >10,000-fold selectivities over the sst sub(2) receptor subtype as well as promising pharmacokinetic properties.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.04.078