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ID: ALA1139995
Journal: Bioorg Med Chem Lett
Title: SAR of the arylpiperazine moiety of obeline somatostatin sst1 receptor antagonists.
Authors: Hurth K, Enz A, Floersheim P, Gentsch C, Hoyer D, Langenegger D, Neumann P, Pfäffli P, Sorg D, Swoboda R, Vassout A, Troxler T.
Abstract: The SAR of over 50 derivatives of octahydrobenzo[g]quinoline (obeline)-type somatostatin sst(1) receptor antagonist 1 is presented, focusing on the modification of its arylpiperazine moiety. Sst(1) affinities in this series cover a range of five orders of magnitude with the best derivatives displaying subnanomolar sst(1) affinities and >10,000-fold selectivities over the sst(2) receptor subtype as well as promising pharmacokinetic properties.
CiteXplore: 17512199