title: Synthesis of galmic: a nonpeptide galanin receptor agonist.
abstract: Galanin is a neuropeptide with a wide variety of biological functions. Few nonpeptide ligands, capable of activating galanin receptors, are available today. Based on known pharmacophores of galanin and the tripeptidomimetic galnon, a combinatorial library was formulated, synthesized, and screened against the galanin receptor. An active compound, galmic, was identified and tested in vitro and in vivo for its affinity and efficacy at galanin receptors. The present work describes the total synthesis of galmic, the synthesis of its oxazole precursors, the coupling of the building blocks into a linear trimer, and the macrolactamization reaction.
authors.affiliation: Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.
authors.forename: Susana Conde
authors.initials: SC
authors.lastname: Ceide
authors.forename: Laurent
authors.initials: L
authors.lastname: Trembleau
authors.forename: Gebhard
authors.initials: G
authors.lastname: Haberhauer
authors.forename: Laszlo
authors.initials: L
authors.lastname: Somogyi
authors.forename: Xiaoying
authors.initials: X
authors.lastname: Lu
authors.forename: Tamas
authors.initials: T
authors.lastname: Bartfai
authors.forename: Julius
authors.initials: J
authors.lastname: Rebek
mesh_terms: D009682:Magnetic Resonance Spectroscopy; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000494:pharmacology; D044088:Receptors, Galanin / Q000819:agonists*; D019032:Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
chemical_list: D010456:Peptides, Cyclic; D044088:Receptors, Galanin; C488574:galmic