Selective angiotensin II AT 2 receptor agonists: Arylbenzylimidazole structure-activity relationships

Xiongyu Wu, Yiqian Wan, A. K. Mahalingam, A. M.S. Murugaiah, Bianca Plouffe, Milad Botros, Anders Karlén, Mathias Hallberg, Nicole Gallo-Payet*, Mathias Alterman

*Corresponding author for this work

Research output: Contribution to journalArticle

37 Citations (Scopus)

Abstract

Structural alterations in the 2- and 5-positions of the first drug-like selective angiotensin II AT 2 receptor agonist (1) have been performed. The imidazole ring system was proven to be a strong determinant for the AT 2 selectivity, and with few exceptions all variations gave good AT 2 receptor affinities and with retained high AT 2 /AT 1 selectivities. On the contrary to the findings with AT 1 receptor agonists, the impact of structural modifications in the 5-position of the AT 2 selective compounds were less pronounced regarding activation of the AT 2 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.

Original languageEnglish
Pages (from-to)7160-7168
Number of pages9
JournalJournal of Medicinal Chemistry
Volume49
Issue number24
DOIs
Publication statusPublished - 30 Nov 2006
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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    Wu, X., Wan, Y., Mahalingam, A. K., Murugaiah, A. M. S., Plouffe, B., Botros, M., Karlén, A., Hallberg, M., Gallo-Payet, N., & Alterman, M. (2006). Selective angiotensin II AT 2 receptor agonists: Arylbenzylimidazole structure-activity relationships. Journal of Medicinal Chemistry, 49(24), 7160-7168. https://doi.org/10.1021/jm0606185