Identification and SAR of potent and selective non-peptide obeline somatostatin sst1 receptor antagonists

被引：7

作者：

Troxler, Thomas ^{[1
]}

Hoyer, Daniel ^{[1
]}

Langenegger, Daniel ^{[1
]}

Neumann, Peter ^{[1
]}

Pfaeffli, Paul ^{[1
]}

Sehoeffter, Philippe ^{[1
]}

Sorg, Dieter ^{[1
]}

Swoboda, Robert ^{[1
]}

Hurth, Konstanze ^{[1
]}

机构：

[1] Novartis Inst Biomed Res, CH-4002 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 14期

关键词：

somatostatin sst(1) receptor antagonists; octa-hydrobenzo[g]quinolines (obelines);

D O I：

10.1016/j.bmcl.2007.04.086

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel class of non-peptide somatostatin receptor ligands bearing the octahydrobenzo[g]quinoline (obeline) structural element has been identified. SAR studies have been performed that led to the discovery of derivatives with high affinity (pK(d) r sst(I) >= 9) and selectivity (>= 150-fold for h sst(1) over h sst(2)-h sst(5)) for somatostatin receptor subtype sst(1). In a functional assay, the compounds act as antagonists at human recombinant sst, receptors. (C) 2007 Elsevier Ltd. All rights reserved.

引用

页码：3983 / 3987

页数：5

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