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Selective angiotensin II AT(2) receptor agonists: Arylbenzylimidazole structure-activity relationships
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry.
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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
Abstract [en]

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.
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Medical and Health Sciences
Identifiers
URN: urn:nbn:se:uu:diva-23504DOI: 10.1021/jm0606185ISI: 000242298000024PubMedID: 17125268OAI: oai:DiVA.org:uu-23504DiVA: diva2:51278
Available from: 2007-01-29 Created: 2007-01-29 Last updated: 2017-12-07Bibliographically approved

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Wu, XiongyuBotros, MiladKarlén, AndersHallberg, Mathias

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