Synthesis of galmic: A nonpeptide galanin receptor agonist

AUTOR(ES)

Ceide, Susana Conde

FONTE

National Academy of Sciences

RESUMO

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.

Documentos Relacionados

• Galmic, a nonpeptide galanin receptor agonist, affects behaviors in seizure, pain, and forced-swim tests
• Anticonvulsant activity of a nonpeptide galanin receptor agonist
• N-terminal galanin-(1-16) fragment is an agonist at the hippocampal galanin receptor.
• A nonpeptide agonist of the invertebrate receptor for SchistoFLRFamide (PDVDHVFLRFamide), a member of a subfamily of insect FMRFamide-related peptides.
• Effect of the nonpeptide thrombopoietin receptor agonist Eltrombopag on bone marrow cells from patients with acute myeloid leukemia and myelodysplastic syndrome