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Rational Design and Synthesis of AT1R Antagonists
Authors:Nikitas Georgiou  Vasileios K. Gkalpinos  Spyridon D. Katsakos  Stamatia Vassiliou  Andreas G. Tzakos  Thomas Mavromoustakos
Affiliation:1.Department of Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis Zografou, 15771 Athens, Greece;2.Department of Chemistry, Section of Organic Chemistry and Biochemistry, University of Ioannina, 45110 Ioannina, Greece; (V.K.G.); (S.D.K.);3.University Research Center of Ioannina (URCI), Institute of Materials Science and Computing, 45110 Ioannina, Greece
Abstract:Hypertension is one of the most common diseases nowadays and is still the major cause of premature death despite of the continuous discovery of novel therapeutics. The discovery of the Renin Angiotensin System (RAS) unveiled a path to develop efficient drugs to fruitfully combat hypertension. Several compounds that prevent the Angiotensin II hormone from binding and activating the AT1R, named sartans, have been developed. Herein, we report a comprehensive review of the synthetic paths followed for the development of different sartans since the discovery of the first sartan, Losartan.
Keywords:sartans   hypertension   AT1R   Angiotensin II   rational design
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