Journal article
SAR of the arylpiperazine moiety of obeline somatostatin sst1 receptor antagonists
K Hurth, A Enz, P Floersheim, C Gentsch, D Hoyer, D Langenegger, P Neumann, P Pfäffli, D Sorg, R Swoboda, A Vassout, T Troxler
Bioorganic and Medicinal Chemistry Letters | PERGAMON-ELSEVIER SCIENCE LTD | Published : 2007
Abstract
The SAR of over 50 derivatives of octahydrobenzo[g]quinoline (obeline)-type somatostatin sst1 receptor antagonist 1 is presented, focusing on the modification of its arylpiperazine moiety. Sst1 affinities in this series cover a range of five orders of magnitude with the best derivatives displaying subnanomolar sst1 affinities and >10,000-fold selectivities over the sst2 receptor subtype as well as promising pharmacokinetic properties. © 2007 Elsevier Ltd. All rights reserved.