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      Selective angiotensin II AT2 receptor agonists: arylbenzylimidazole structure-activity relationships.

      Journal of Medicinal Chemistry
      Animals, Benzimidazoles, chemical synthesis, chemistry, pharmacology, Cell Differentiation, drug effects, Cell Line, Tumor, Female, Ligands, Liver, metabolism, Neurites, physiology, Radioligand Assay, Rats, Receptor, Angiotensin, Type 2, agonists, Structure-Activity Relationship, Sulfonamides, Swine, Thiophenes, Uterus

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          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.

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