Structure elucidation and conformational study of V8: a novel synthetic non peptide AT(1) antagonist

AT(1) antagonists constitute the most recent class of antihypertensive drugs which act through the Renin Angiotensin System (RAS). In an effort to comprehend their stereoelectronic features, a study was initiated to compare the conformational properties of drugs already marketed for the treatment of...

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Published inJournal of pharmaceutical and biomedical analysis Vol. 40; no. 5; pp. 1097 - 1104
Main Authors Zoumpoulakis, Panagiotis, Politi, Aggeliki, Grdadolnik, Simona Golic, Matsoukas, John, Mavromoustakos, Thomas
Format Journal Article
LanguageEnglish
Published England 18.03.2006
Subjects
Angiotensin II Type 1 Receptor Blockers - analysis
Angiotensin II Type 1 Receptor Blockers - chemistry
Biphenyl Compounds - chemistry
Dimethyl Sulfoxide
Imidazoles - chemistry
Losartan - analogs & derivatives
Losartan - analysis
Losartan - chemistry
Magnetic Resonance Spectroscopy
Models, Molecular
Molecular Conformation
Monte Carlo Method
Tetrazoles - chemistry
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Summary:AT(1) antagonists constitute the most recent class of antihypertensive drugs which act through the Renin Angiotensin System (RAS). In an effort to comprehend their stereoelectronic features, a study was initiated to compare the conformational properties of drugs already marketed for the treatment of hypertension with synthetic ones, possessing common structural characteristics. In this study, the synthetic AT(1) antagonist V8 is structurally elucidated and its conformational properties are studied through a combination of NMR spectroscopy and computational analysis. Its conformational properties are compared with those of the structurally similar prototype AT(1) antagonist losartan.
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ISSN:0731-7085
DOI:10.1016/j.jpba.2005.09.016