Journal article
SAR of the arylpiperazine moiety of obeline somatostatin sst(1) receptor antagonists
Konstanze Hurth, Albert Enz, Philipp Floersheim, Conrad Gentsch, Daniel Hoyer, Daniel Langenegger, Peter Neumann, Paul Pfaeffli, Dieter Sorg, Robert Swoboda, Annick Vassout, Thomas Troxler
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | PERGAMON-ELSEVIER SCIENCE LTD | Published : 2007
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.