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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.

SUBMITTER: Ceide SC

PROVIDER: S-EPMC534730 | biostudies-literature | 2004 Nov

REPOSITORIES: biostudies-literature

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Synthesis of galmic: a nonpeptide galanin receptor agonist.

Ceide Susana Conde SC Trembleau Laurent L Haberhauer Gebhard G Somogyi Laszlo L Lu Xiaoying X Bartfai Tamas T Rebek Julius J

Proceedings of the National Academy of Sciences of the United States of America 20041119 48

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 synthesi ...[more]

PMID: 15557002

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