An update on non-peptide angiotensin receptor antagonists and related RAAS modulators

Life Sciences
G K AulakhManjeet Singh

Abstract

The renin-angiotensin-aldosterone-system (RAAS) is an important regulator of blood pressure and fluid-electrolyte homeostasis. RAAS has been implicated in pathogenesis of hypertension, congestive heart failure, and chronic renal failure. Aliskiren is the first non-peptide orally active renin inhibitor approved by FDA. Angiotensin Converting Enzyme (ACE) Inhibitors are associated with frequent side effects such as cough and angio-oedema. Recently, the role of ACE2 and neutral endopeptidase (NEP) in the formation of an important active metabolite/mediator of RAAS, ang 1-7, has initiated attempts towards development of ACE2 inhibitors and combined ACE/NEP inhibitors. Furukawa and colleagues developed a series of low molecular weight nonpeptide imidazole analogues that possess weak but selective, competitive AT1 receptor blocking property. Till date, many compounds have exhibited promising AT1 blocking activity which cause a more complete RAAS blockade than ACE inhibitors. Many have reached the market for alternative treatment of hypertension, heart failure and diabetic nephropathy in ACE inhibitor intolerant patients and still more are waiting in the queue. But, the hallmark of this area of drug research is marked by a progress in...Continue Reading

References

Mar 27, 1975·The New England Journal of Medicine·D H StreetenT G Dalakos
Aug 22, 1977·JAMA : the Journal of the American Medical Association·H GavrasI Gavras
Jul 21, 1992·European Journal of Pharmacology·J ZhangJ C Van Meel
Apr 1, 1991·Hypertension·N E RhalebD Regoli
Nov 11, 1991·Hypertension·P B TimmermansA L Johnson
Jan 1, 1991·Advances in Pharmacology·H D KleinertH H Stein
May 31, 1991·Biochemical and Biophysical Research Communications·A T ChiuP B Timmermans
Jan 1, 1989·Cardiology·J NussbergerH R Brunner
Aug 30, 1989·Biochemical and Biophysical Research Communications·S WhitebreadM de Gasparo
Nov 15, 1988·European Journal of Pharmacology·A T ChiuP B Timmermans
May 30, 1985·The New England Journal of Medicine·J A LuetscherM Bryer-Ash
Apr 28, 1995·European Journal of Pharmacology·M FleschA Sachinidis
Jan 1, 1995·Journal of Cardiovascular Pharmacology·S MochizukiA Tomiyama
May 1, 1995·Hypertension·M de GasparoP B Timmermans
Apr 1, 1995·Kidney International·S ShanmugamC M Llorens-Cortes
Oct 1, 1994·Trends in Pharmacological Sciences·M J RobertsonP Leff
Jan 1, 1994·Current Opinion in Nephrology and Hypertension·R D Smith, P B Timmermans
Jan 1, 1994·British Journal of Pharmacology·A HilditchM J Robertson
Dec 10, 1993·Journal of Medicinal Chemistry·M K VanAttenP B Timmermans
Oct 16, 1995·European Journal of Pharmacology·M MizunoH Koike
Aug 30, 1996·Molecular and Cellular Endocrinology·S MeffertT Unger
Jan 1, 1997·Clinical Pharmacokinetics·C CsajkaJ Biollaz
Dec 5, 1997·Journal of Cardiovascular Pharmacology·K TamuraK Hashimoto
Apr 1, 1995·Molecular Medicine Today·G P VinsonJ R Puddefoot
May 20, 1998·Drugs·K J McClellan, J A Balfour
Sep 12, 1998·Lancet·J NussbergerA Agostoni

❮ Previous
Next ❯

Citations

Nov 26, 2009·Pediatric Nephrology : Journal of the International Pediatric Nephrology Association·Siegtraut Dorothea HerderHartmut Morck
Jan 25, 2013·American Journal of Cardiovascular Drugs : Drugs, Devices, and Other Interventions·Jeong Bae ParkEun Joo Cho
Oct 5, 2013·Journal of Chemical Information and Modeling·Minos-Timotheos MatsoukasTheodore Tselios
Oct 12, 2012·Hypertension Research : Official Journal of the Japanese Society of Hypertension·Daisuke UenoHironobu Yoshimatsu
Jan 9, 2010·Annual Review of Pharmacology and Toxicology·Michael Bader
Jul 3, 2013·Biological & Pharmaceutical Bulletin·Yong Ha ChiKyung-Tae Lee
Dec 24, 2011·Journal of the American Society of Nephrology : JASN·Dong LiAnita Aperia
Feb 21, 2009·Journal of Periodontology·C F SantosM C O Salgado
Dec 5, 2015·The Journal of Organic Chemistry·Alexei V Buevich
Mar 19, 2016·Journal of the American Chemical Society·Tejas K ShahNeil K Garg
Apr 1, 2014·Neuroscience Letters·Junjun LiuHiroto Komano
Jul 1, 2014·Clinical and Experimental Nephrology·Takako NagaiKeizo Kanasaki
Jul 14, 2017·Organic Letters·Giovanni Di MauroNuno Maulide
May 22, 2009·Expert Opinion on Therapeutic Patents·David W Laight
Dec 4, 2009·Expert Review of Cardiovascular Therapy·Yves LacourcièreRita Samuel
Aug 25, 2017·Expert Opinion on Investigational Drugs·Santiago Perez-LloretFrancisco Capani
Jan 25, 2021·Drug Discovery Today·Antonio VitielloFrancesco Ferrara
Mar 9, 2021·The Journal of Organic Chemistry·Andrea M NikolićIgor M Opsenica
Dec 2, 2017·Journal of Chemical Information and Modeling·Khuraijam Dhanachandra SinghSadashiva S Karnik
Nov 13, 2010·Bioorganic & Medicinal Chemistry·Prashant NaikMange Ram Yadav

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