Selective angiotensin II AT(2) receptor agonists: Arylbenzylimidazole structure-activity relationships
2006 (English)In: Journal of Medicinal Chemistry, ISSN 0022-2623, E-ISSN 1520-4804, Vol. 49, no 24, 7160-7168 p.Article in journal (Refereed) Published
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.
Place, publisher, year, edition, pages
2006. Vol. 49, no 24, 7160-7168 p.
Medical and Health Sciences
IdentifiersURN: urn:nbn:se:uu:diva-23504DOI: 10.1021/jm0606185ISI: 000242298000024PubMedID: 17125268OAI: oai:DiVA.org:uu-23504DiVA: diva2:51278