Selective angiotensin II AT 2 receptor agonists devoid of the imidazole ring system

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

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

29 Citations (Scopus)


A versatile parallel synthetic method to obtain three series of non-cyclic analogues of the first drug-like selective angiotensin II AT 2 receptor agonist (1) has been developed. In analogy with the transformation of losartan to valsartan it was demonstrated that a non-cyclic moiety could be employed as an imidazole replacement to obtain AT 2 selective compounds. In all the three series, AT 2 receptor ligands with affinities in the lower nanomolar range were found. None of the analogues exhibited any affinity for the AT 1 receptor. Four compounds, 17, 22, 39 and 51, were examined in a neurite outgrowth cell assay. All four compounds 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)7166-7183
Number of pages18
JournalBioorganic and Medicinal Chemistry
Issue number22
Publication statusPublished - 15 Nov 2007
Externally publishedYes


  • Agonist
  • Angiotensin
  • AT

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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