SAR of the arylpiperazine moiety of obeline somatostatin sst1 receptor antagonists

Bioorg Med Chem Lett. 2007 Jul 15;17(14):3988-91. doi: 10.1016/j.bmcl.2007.04.078. Epub 2007 Apr 30.


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.

MeSH terms

  • Luminescent Proteins / chemistry
  • Luminescent Proteins / pharmacology*
  • Piperazines / chemistry
  • Piperazines / pharmacology*
  • Receptors, Somatostatin / antagonists & inhibitors*
  • Structure-Activity Relationship


  • Luminescent Proteins
  • Piperazines
  • Receptors, Somatostatin
  • obelin