Journal article
Novel paramagnetic AT1 receptor antagonists
NPH Tan, MK Taylor, SE Bottle, CE Wright, J Ziogas, JM White, CH Schiesser, NV Jani
Chemical Communications | ROYAL SOC CHEMISTRY | Published : 2011
DOI: 10.1039/c1cc14920b
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 pKB 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. © The Royal Society of Chemistry 2011.
Grants
Funding Acknowledgements
We thank the Australian Research Council through the Centres of Excellence Scheme for generous financial support.