Rational Design and Synthesis of AT1R Antagonists.

Nikitas Georgiou, Vasileios K Gkalpinos, Spyridon D Katsakos, Stamatia Vassiliou, Andreas G Tzakos, Thomas Mavromoustakos

Molecules (Basel, Switzerland) 2021 May 14

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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.

Citation

Nikitas Georgiou, Vasileios K Gkalpinos, Spyridon D Katsakos, Stamatia Vassiliou, Andreas G Tzakos, Thomas Mavromoustakos. Rational Design and Synthesis of AT1R Antagonists. Molecules (Basel, Switzerland). 2021 May 14;26(10)