Novel paramagnetic AT₁ receptor antagonists

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

doi:10.1039/c1cc14920b

Novel paramagnetic AT₁ receptor antagonists

Nichole PH Tan
, Michelle K Taylor
, Steven E Bottle
, Christine E Wright
, James Ziogas
, Jonathan M White
, Carl H Schiesser
, Natya V Jani

Chemistry

Research output: Contribution to journal › Article › peer-review

9 Citations (Scopus)

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.

Original language	English
Pages (from-to)	12083-12085
Journal	Chemical Communications
Volume	47
Issue number	44
DOIs	https://doi.org/10.1039/c1cc14920b
Publication status	Published - 2011

Keywords

Biologically Active Molecules
Organic Chemical Synthesis

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10.1039/c1cc14920b

https://hdl.handle.net/1959.11/9560

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title = "Novel paramagnetic AT₁ receptor antagonists",

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.",

keywords = "Biologically Active Molecules, Organic Chemical Synthesis",

author = "Tan, \{Nichole PH\} and Taylor, \{Michelle K\} and Bottle, \{Steven E\} and Wright, \{Christine E\} and James Ziogas and White, \{Jonathan M\} and Schiesser, \{Carl H\} and Jani, \{Natya V\}",

year = "2011",

doi = "10.1039/c1cc14920b",

language = "English",

volume = "47",

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journal = "Chemical Communications",

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publisher = "Royal Society of Chemistry",

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T1 - Novel paramagnetic AT₁ receptor antagonists

AU - Tan, Nichole PH

AU - Taylor, Michelle K

AU - Bottle, Steven E

AU - Wright, Christine E

AU - Ziogas, James

AU - White, Jonathan M

AU - Schiesser, Carl H

AU - Jani, Natya V

PY - 2011

Y1 - 2011

N2 - 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.

AB - 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.

KW - Biologically Active Molecules

KW - Organic Chemical Synthesis

U2 - 10.1039/c1cc14920b

DO - 10.1039/c1cc14920b

M3 - Article

SN - 1359-7345

VL - 47

SP - 12083

EP - 12085

JO - Chemical Communications

JF - Chemical Communications

IS - 44

ER -

Novel paramagnetic AT₁ receptor antagonists

Abstract

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