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Synthesis and evaluation of isoleucine derived angiotensin II AT(2) receptor ligands
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Organic Pharmaceutical Chemistry.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Organic Pharmaceutical Chemistry.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Organic Pharmaceutical Chemistry.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Organic Pharmaceutical Chemistry.
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2014 (English)In: Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, E-ISSN 1090-2120, Vol. 24, no 2, 476-479 p.Article in journal (Refereed) Published
Abstract [en]

Sixteen new C-terminally modified analogues of 2, a previously described potent and selective AT(2)R ligand, were designed, synthesized and evaluated for their affinity to the AT(2)R receptor. The introduction of large, hydrophobic substituents was shown to be beneficial and the most active compound (17, K-i = 8.5 mu M) was over 12-times more potent than the lead compound 2.

Place, publisher, year, edition, pages
2014. Vol. 24, no 2, 476-479 p.
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Natural Sciences Basic Medicine
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URN: urn:nbn:se:uu:diva-217652DOI: 10.1016/j.bmcl.2013.12.040ISI: 000329430600013OAI: oai:DiVA.org:uu-217652DiVA: diva2:695777
Available from: 2014-02-12 Created: 2014-02-04 Last updated: 2017-12-06Bibliographically approved

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Wallinder, CharlottaLarhed, MatsOdell, Luke R.

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