Rational Design and Synthesis of AT1R Antagonists

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. Severa...

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Main Authors: Nikitas Georgiou, Vasileios K. Gkalpinos, Spyridon D. Katsakos, Stamatia Vassiliou, Andreas G. Tzakos, Thomas Mavromoustakos
Format: Article
Language:English
Published: MDPI AG 2021-05-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/26/10/2927
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author Nikitas Georgiou
Vasileios K. Gkalpinos
Spyridon D. Katsakos
Stamatia Vassiliou
Andreas G. Tzakos
Thomas Mavromoustakos
author_facet Nikitas Georgiou
Vasileios K. Gkalpinos
Spyridon D. Katsakos
Stamatia Vassiliou
Andreas G. Tzakos
Thomas Mavromoustakos
author_sort Nikitas Georgiou
collection DOAJ
description 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.
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spelling doaj.art-b0376ac87769412f8da28c80a864ef722023-11-21T19:46:41ZengMDPI AGMolecules1420-30492021-05-012610292710.3390/molecules26102927Rational Design and Synthesis of AT1R AntagonistsNikitas Georgiou0Vasileios K. Gkalpinos1Spyridon D. Katsakos2Stamatia Vassiliou3Andreas G. Tzakos4Thomas Mavromoustakos5Department of Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis Zografou, 15771 Athens, GreeceDepartment of Chemistry, Section of Organic Chemistry and Biochemistry, University of Ioannina, 45110 Ioannina, GreeceDepartment of Chemistry, Section of Organic Chemistry and Biochemistry, University of Ioannina, 45110 Ioannina, GreeceDepartment of Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis Zografou, 15771 Athens, GreeceDepartment of Chemistry, Section of Organic Chemistry and Biochemistry, University of Ioannina, 45110 Ioannina, GreeceDepartment of Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis Zografou, 15771 Athens, GreeceHypertension 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.https://www.mdpi.com/1420-3049/26/10/2927sartanshypertensionAT1RAngiotensin IIrational design
spellingShingle Nikitas Georgiou
Vasileios K. Gkalpinos
Spyridon D. Katsakos
Stamatia Vassiliou
Andreas G. Tzakos
Thomas Mavromoustakos
Rational Design and Synthesis of AT1R Antagonists
Molecules
sartans
hypertension
AT1R
Angiotensin II
rational design
title Rational Design and Synthesis of AT1R Antagonists
title_full Rational Design and Synthesis of AT1R Antagonists
title_fullStr Rational Design and Synthesis of AT1R Antagonists
title_full_unstemmed Rational Design and Synthesis of AT1R Antagonists
title_short Rational Design and Synthesis of AT1R Antagonists
title_sort rational design and synthesis of at1r antagonists
topic sartans
hypertension
AT1R
Angiotensin II
rational design
url https://www.mdpi.com/1420-3049/26/10/2927
work_keys_str_mv AT nikitasgeorgiou rationaldesignandsynthesisofat1rantagonists
AT vasileioskgkalpinos rationaldesignandsynthesisofat1rantagonists
AT spyridondkatsakos rationaldesignandsynthesisofat1rantagonists
AT stamatiavassiliou rationaldesignandsynthesisofat1rantagonists
AT andreasgtzakos rationaldesignandsynthesisofat1rantagonists
AT thomasmavromoustakos rationaldesignandsynthesisofat1rantagonists