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- Title
Small‐molecule AT2 receptor agonists.
- Authors
Hallberg, Mathias; Sumners, Colin; Steckelings, U. Muscha; Hallberg, Anders
- Abstract
Abstract: The discovery of the first selective, small‐molecule ATR receptor (AT2R) agonist compound 21 (C21) (<bold>8</bold>) that is now extensively studied in a large variety of in vitro and in vivo models is described. The sulfonylcarbamate derivative <bold>8</bold>, encompassing a phenylthiofen scaffold is the drug‐like agonist with the highest affinity for the AT2R reported to date (<italic>K</italic>i = 0.4 nM). Structure‐activity relationships (SAR), regarding different biaryl scaffolds and functional groups attached to these scaffolds and with a particular focus on the impact of various <italic>para</italic> substituents displacing the methylene imidazole group of <bold>8</bold>, are discussed. Furthermore, the consequences of migration of the methylene imidazole group and presumed structural requirements for ligands that are aimed as AT2R agonists (e.g. <bold>8</bold>) or AT2R antagonists (e.g. <bold>9</bold>), respectively, are briefly addressed. A summary of the pharmacological actions of C21 (<bold>8</bold>) is also presented.
- Publication
Medicinal Research Reviews, 2018, Vol 38, Issue 2, p602
- ISSN
0198-6325
- Publication type
Article
- DOI
10.1002/med.21449