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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Malik L,Kelly NM,Ma JN,Currier EA,Burstein ES,Olsson R

doi

10.1016/j.bmcl.2009.01.085

subject

Has Abstract

pub_date

2009-03-15 00:00:00

pages

1729-32

issue

6

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(09)00120-6

journal_volume

19

pub_type

杂志文章

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