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

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• 作者：Leila Malik ; Nicholas M. Kelly ; Jian-Nong Ma ; Erika A. Currier ; Ethan S. Burstein ; Roger Olsson
• 关键词：Mas related ; MrgX1 ; MrgX2 ; Agonist ; SNSR ; Sensory-neuron specific receptors ; Nociception ; Non-peptidergic ; Small molecule ; Solid-phase ; R-SAT
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2009
• 出版时间：15 March 2009
• 年：2009
• 卷：19
• 期：6
• 页码：1729-1732
• 全文大小：1573 K

文摘

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.