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.
MeSH terms
-
Animals
-
Benzimidazoles / chemistry
-
Cattle
-
Chemistry, Pharmaceutical / methods*
-
Combinatorial Chemistry Techniques
-
Drug Design
-
Humans
-
Intercellular Signaling Peptides and Proteins
-
Ligands
-
Macaca mulatta
-
Models, Chemical
-
Nerve Tissue Proteins / agonists*
-
Nerve Tissue Proteins / chemistry*
-
Peptides / chemistry
-
Receptors, G-Protein-Coupled / agonists*
-
Receptors, G-Protein-Coupled / chemistry*
-
Receptors, Neuropeptide / agonists*
-
Receptors, Neuropeptide / chemistry*
-
Structure-Activity Relationship
Substances
-
Benzimidazoles
-
Intercellular Signaling Peptides and Proteins
-
Ligands
-
MRGPRX2 protein, human
-
Nerve Tissue Proteins
-
Peptides
-
Receptors, G-Protein-Coupled
-
Receptors, Neuropeptide
-
mas-related gene-X1 receptor, human
-
corticostatin