title: SAR of the arylpiperazine moiety of obeline somatostatin sst1 receptor antagonists.
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.
authors.affiliation: Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland. konstanze.hurth@novartis.com
authors.forename: Konstanze
authors.initials: K
authors.lastname: Hurth
authors.forename: Albert
authors.initials: A
authors.lastname: Enz
authors.forename: Philipp
authors.initials: P
authors.lastname: Floersheim
authors.forename: Conrad
authors.initials: C
authors.lastname: Gentsch
authors.forename: Daniel
authors.initials: D
authors.lastname: Hoyer
authors.forename: Daniel
authors.initials: D
authors.lastname: Langenegger
authors.forename: Peter
authors.initials: P
authors.lastname: Neumann
authors.forename: Paul
authors.initials: P
authors.lastname: Pfäffli
authors.forename: Dieter
authors.initials: D
authors.lastname: Sorg
authors.forename: Robert
authors.initials: R
authors.lastname: Swoboda
authors.forename: Annick
authors.initials: A
authors.lastname: Vassout
authors.forename: Thomas
authors.initials: T
authors.lastname: Troxler
mesh_terms: D008164:Luminescent Proteins / Q000737:chemistry / Q000494:pharmacology*; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology*; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D008164:Luminescent Proteins; D010879:Piperazines; D017481:Receptors, Somatostatin; C010497:obelin