SAR of the arylpiperazine moiety of obeline somatostatin sst1 receptor antagonists.

Konstanze Hurth,Albert Enz,Philipp Floersheim,Conrad Gentsch,Daniel Hoyer,Daniel Langenegger,Peter Neumann,Paul Pfäffli,Dieter Sorg,Robert Swoboda,Annick Vassout,Thomas Troxler

Bioorganic & Medicinal Chemistry Letters（2007）

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摘要

The optimization of the arylpiperazine moiety in obeline-type somatostatin sst1 antagonists is presented, leading to compounds with subnanomolar sst1 affinities and >10,000-fold selectivities over the sst2 receptor subtype as well as promising pharmacokinetic properties.

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关键词

Somatostatin sst1 receptor antagonist,Octahydro[g]quinoline (obeline)

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