Selective angiotensin II AT2 receptor agonists: Benzamide structure–activity relationships

In the investigation of the structure–activity relationship of nonpeptide AT2 receptor agonists, a series of substituted benzamide analogues of the selective nonpeptide AT2 receptor agonist M024 have been synthesised. In a second series, the biphenyl scaffold was compared to the thienylphenyl scaffold and the impact of the isobutyl substituent and its position on AT1/AT2 receptor selectivity was also investigated. Both series included several compounds with high affinity and selectivity for the AT2 receptor. Three of the compounds were also proven to function as agonists at the AT2 receptor, as deduced from a neurite outgrowth assay, conducted in NG108-15 cells.

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