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Selective angiotensin II AT(2) receptor agonists with reduced CYP 450 inhibition
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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2010 (English)In: Bioorganic & Medicinal Chemistry, ISSN 0968-0896, E-ISSN 1464-3391, Vol. 18, no 12, 4570-4590 p.Article in journal (Refereed) Published
Abstract [en]

Structural alterations to the benzylic position of the first drug-like selective angiotensin II AT(2) receptor agonist (1) have been performed, with the emphasis to reduce the CYP 450 inhibitory property of the initial structure. The imidazole moiety, responsible for the CYP 450 inhibitory effect in 1, was replaced with various heterocycles. In addition, the modes of attachment of the heterocycles, that is, carbon versus nitrogen attachment, and introduction of carbonyl functionalities to the benzylic position have been evaluated. In all the three series, AT(2) receptor ligands with affinity in the lower nanomolar range were identified. None of the analogues, regardless of the substituents, exhibited any affinity for the AT(1) receptor. Compounds with substantially reduced inhibition of the CYP 450 enzymes were obtained. Among them the compound 60 was found to induce neurite elongation in NG 108-15 cells and served as potent AT(2) selective agonist.

Place, publisher, year, edition, pages
2010. Vol. 18, no 12, 4570-4590 p.
Keyword [en]
Angiotesin, AT(2), Agonist
National Category
Pharmaceutical Sciences
Identifiers
URN: urn:nbn:se:uu:diva-136054DOI: 10.1016/j.bmc.2010.03.064ISI: 000278480900044PubMedID: 20493713OAI: oai:DiVA.org:uu-136054DiVA: diva2:376116
Available from: 2010-12-10 Created: 2010-12-09 Last updated: 2017-12-11

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Wallinder, Charlotta

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