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N-Aryl Isoleucine Derivatives as 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.
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2014 (English)In: ChemistryOpen, ISSN 2191-1363, Vol. 3, no 2, 65-75 p.Article in journal (Refereed) Published
Abstract [en]

A novel series of ligands for the recombinant human AT(2) receptor has been synthesized utilizing a fast and efficient palladium-catalyzed procedure for aminocarbonylation as the key reaction. Molybdenum hexacarbonyl [Mo(CO)(6)] was employed as the carbon monoxide source, and controlled microwave heating was applied. The prepared N-aryl isoleucine derivatives, encompassing a variety of amide groups attached to the aromatic system, exhibit binding affinities at best with K-i values in the low micromolar range versus the recombinant human AT(2) receptor. Some of the new nonpeptidic isoleucine derivatives may serve as starting points for further structural optimization. The presented data emphasize the importance of using human receptors in drug discovery programs.

Place, publisher, year, edition, pages
2014. Vol. 3, no 2, 65-75 p.
Keyword [en]
aminocarbonylation, AT(2) receptor, medicinal chemistry, palladium catalysis, peptide mimics
National Category
Medicinal Chemistry
Identifiers
URN: urn:nbn:se:uu:diva-225073DOI: 10.1002/open.201300040ISI: 000334680800004OAI: oai:DiVA.org:uu-225073DiVA: diva2:727254
Available from: 2014-06-19 Created: 2014-05-27 Last updated: 2017-12-05Bibliographically approved

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