title: Discovery of novel non-peptidic beta-alanine piperazine amide derivatives and their optimization to achiral, easily accessible, potent and selective somatostatin sst1 receptor antagonists.
abstract: Structural simplification of the core moieties of obeline and ergoline somatostatin sst(1) receptor antagonists, followed by systematic optimization, led to the identification of novel, highly potent and selective sst(1) receptor antagonists. These achiral, non-peptidic compounds are easily prepared and show promising PK properties in rodents.
authors.affiliation: Novartis Institutes for BioMedical Research, Neuroscience Chemistry, WSJ-088.3.06, CH-4002 Basel, BS, Switzerland.
authors.forename: Thomas
authors.initials: T
authors.lastname: Troxler
authors.forename: Konstanze
authors.initials: K
authors.lastname: Hurth
authors.forename: Henri
authors.initials: H
authors.lastname: Mattes
authors.forename: Mahavir
authors.initials: M
authors.lastname: Prashad
authors.forename: Philippe
authors.initials: P
authors.lastname: Schoeffter
authors.forename: Daniel
authors.initials: D
authors.lastname: Langenegger
authors.forename: Albert
authors.initials: A
authors.lastname: Enz
authors.forename: Daniel
authors.initials: D
authors.lastname: Hoyer
mesh_terms: D000818:Animals; D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery; D006801:Humans; D051379:Mice; D000077489:Piperazine; D010879:Piperazines / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D011485:Protein Binding; D051381:Rats; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors* / Q000502:physiology; D013237:Stereoisomerism; D015091:beta-Alanine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology
chemical_list: D010879:Piperazines; D017481:Receptors, Somatostatin; C101130:somatostatin receptor type 1; D015091:beta-Alanine; D000077489:Piperazine; C012731:beta-alanine amide