Synthesis of galmic : A non-peptide galanin receptor agonist
In: Proceedings of the National Academy of Sciences of the United States of America (PNAS), Vol. 101 (2004), No. 48, pp. 16727 - 16732
Title in English:
Synthesis of galmic : A non-peptide galanin receptor agonist
Author:
Ceide, Susana Conde;Trembleau, Laurent;Haberhauer, GebhardUDE
- LSF ID
- 14720
- ORCID
- 0000-0002-5427-7510
- Other
- connected with university
Year of publication:
2004
Open Access?:
Open Access
Language of text:
English
Abstract:
Galanin is a neuropeptide with a wide variety of biol. functions. Few non-peptide 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 compd., galmic (I), 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 I, the synthesis of its oxazole precursors, the coupling of the building blocks into a linear trimer, and the macrolactamization reaction.