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Novel paramagnetic AT1 receptor antagonists

机译：新型顺磁性AT1受体拮抗剂

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摘要

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.
机译：已经制备了带有氮氧化物（3，4）的新型顺磁性选择性血管紧张素AT_1受体拮抗剂（sartans），并在体内和体外评估了它们的药理作用。化合物3,4被证明是有效的沙坦，pK_B估计在6.2-9.1范围内。此外，钠盐（11）为4（R = Bu）能够预防高血压大鼠的血管损伤，这取决于其减弱由颈动脉球囊损伤引起的内膜增厚发展的能力。

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  • 来源
    《Chemical Communications》 |2011年第44期|p.12083-12085|共3页
  • 作者

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

  • 作者单位

    ARC Centre of Excellence for Free Radical Chemistry and Biotechnology, Victoria, Australia,School of Chemistry and Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Victoria, 3010, Australia;

    ARC Centre of Excellence for Free Radical Chemistry and Biotechnology, Victoria, Australia,School of Chemistry and Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Victoria, 3010, Australia;

    ARC Centre of Excellence for Free Radical Chemistry and Biotechnology, Victoria, Australia,School of Physical and Chemical Sciences, Queensland University of Technology, GPO Box 2432, Brisbane, QLD 4001, Australia;

    ARC Centre of Excellence for Free Radical Chemistry and Biotechnology, Victoria, Australia,Department of Pharmacology, The University of Melbourne,Victoria, 3010, Australia;

    ARC Centre of Excellence for Free Radical Chemistry and Biotechnology, Victoria, Australia,Department of Pharmacology, The University of Melbourne,Victoria, 3010, Australia;

    School of Chemistry and Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Victoria, 3010, Australia;

    ARC Centre of Excellence for Free Radical Chemistry and Biotechnology, Victoria, Australia,School of Chemistry and Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Victoria, 3010, Australia;

    ARC Centre of Excellence for Free Radical Chemistry and Biotechnology, Victoria, Australia,Department of Pharmacology, The University of Melbourne,Victoria, 3010, Australia;

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  • 入库时间 2022-08-17 13:22:55

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