Novel paramagnetic AT1 receptor antagonists |
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| Authors: | Tan Nichole P H Taylor Michelle K Bottle Steven E Wright Christine E Ziogas James White Jonathan M Schiesser Carl H Jani Nitya V |
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| Affiliation: | ARC Centre of Excellence for Free Radical Chemistry and Biotechnology, Victoria, Australia. |
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| Abstract: | Novel paramagnetic selective angiotensin AT(1) 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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