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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MDPI AG
2021-05-01
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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. |
first_indexed | 2024-03-10T11:25:06Z |
format | Article |
id | doaj.art-b0376ac87769412f8da28c80a864ef72 |
institution | Directory Open Access Journal |
issn | 1420-3049 |
language | English |
last_indexed | 2024-03-10T11:25:06Z |
publishDate | 2021-05-01 |
publisher | MDPI AG |
record_format | Article |
series | Molecules |
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 |