Novel paramagnetic AT1 receptor antagonists

Nichole P. H. Tan; Michelle K. Taylor; Steven E. Bottle; Christine E. Wright; James Ziogas; Jonathan M. White; Carl H. Schiesser; Nitya V. Jani

doi:10.1039/C1CC14920B

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Novel paramagnetic AT₁ receptor antagonists†

Nichole P. H. Tan,^ab Michelle K. Taylor,‡^ab Steven E. Bottle,^ac Christine E. Wright,^ad James Ziogas,^ad Jonathan M. White,^b Carl H. Schiesser*^ab and Nitya V. Jani*^ad

Author affiliations

* Corresponding authors

^a ARC Centre of Excellence for Free Radical Chemistry and Biotechnology, Victoria, Australia

^b School of Chemistry and Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Victoria, Australia
E-mail: carlhs@unimelb.edu.au
Fax: +61 3 9347 8189
Tel: +61 3 8344 2432

^c School of Physical and Chemical Sciences, Queensland University of Technology, GPO Box 2432, Brisbane, QLD, Australia

^d Department of Pharmacology, The University of Melbourne, Victoria, Australia

Abstract

Novel paramagnetic selective angiotensin AT₁ receptor antagonists (sartans) bearing nitroxides (3, 4) have been prepared and their pharmacology evaluated in vitro as well as in vivo. Compounds 3, 4 proved to be effective sartans with pK_B estimates in the range 6.2–9.1. In addition, the sodium salt (11) of 4 (R = Bu) is able to protect against vascular injury in hypertensive rats as determined by its ability to attenuate the development of intimal thickening caused by balloon injury of the carotid artery.

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Article information

DOI: https://doi.org/10.1039/C1CC14920B
Article type: Communication
Submitted: 09 Aug 2011
Accepted: 21 Sep 2011
First published: 30 Sep 2011

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Chem. Commun., 2011,47, 12083-12085

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Novel paramagnetic AT₁ receptor antagonists

N. P. H. Tan, M. K. Taylor, S. E. Bottle, C. E. Wright, J. Ziogas, J. M. White, C. H. Schiesser and N. V. Jani, Chem. Commun., 2011, 47, 12083 DOI: 10.1039/C1CC14920B

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