Selective angiotensin II AT2 receptor agonists: arylbenzylimidazole structure-activity relationships.
Basic Information
ID: ALA1137349
Journal: J Med Chem
Title: Selective angiotensin II AT2 receptor agonists: arylbenzylimidazole structure-activity relationships.
Authors: Wu X, Wan Y, Mahalingam AK, Murugaiah AM, Plouffe B, Botros M, Karlén A, Hallberg M, Gallo-Payet N, Alterman M.
Abstract: Structural alterations in the 2- and 5-positions of the first drug-like selective angiotensin II AT2 receptor agonist (1) have been performed. The imidazole ring system was proven to be a strong determinant for the AT2 selectivity, and with few exceptions all variations gave good AT2 receptor affinities and with retained high AT2/AT1 selectivities. On the contrary to the findings with AT1 receptor agonists, the impact of structural modifications in the 5-position of the AT2 selective compounds were less pronounced regarding activation of the AT2 receptor. The butyloxyphenyl (56) and the propylthienyl (50) derivatives were found to exert a high agonistic effect as deduced from their capacity to induce neurite elongation in neuronal cells, as does angiotensin II.
CiteXplore: 17125268
DOI: 10.1021/jm0606185
Patent ID: ┄