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Bioorg Med Chem Lett. 2009 Mar 15;19(6):1729-32. doi: 10.1016/j.bmcl.2009.01.085. Epub 2009 Jan 30.

Discovery of non-peptidergic MrgX1 and MrgX2 receptor agonists and exploration of an initial SAR using solid-phase synthesis.

Author information

1
ACADIA Pharmaceuticals AB, Medeon Science Park, S-205 12 Malmö, Sweden.

Abstract

A class of small molecules displaying comparable activities with peptide ligands BAM22 and corticostatin-14 at both the human and rhesus monkey MrgX1 and MrgX2 receptors, respectively, was discovered. A comparative study to compare solid-phase and solution-phase chemistries for the efficient synthesis of the active class, tetracyclic benzimidazoles, was undertaken. The solid-phase chemistry was found to be superior both for the synthesis of analogs and for the synthesis of gram quantities.

PMID:
19230660
DOI:
10.1016/j.bmcl.2009.01.085
[Indexed for MEDLINE]

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