Design and synthesis of nonpeptide angiotensin II receptor antagonists featuring acyclic imidazole-mimicking structural units

Extensive molecular modelling studies, including conformational analysis and the comparison of molecular electrostatic potential distributions, were used to evaluate structural parameters of new antagonists containing acyclic replacements of the N=C-N imidazole region. The synthesis and the biologic...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 1998-11, Vol.6 (11), p.2013-2027
Main Authors: Angiolini, Mauro, Belvisi, Laura, Poma, Davide, Salimbeni, Aldo, Sciammetta, Nunzio, Scolastico, Carlo
Format: Article
Language:English
Subjects:
Angiotensin Receptor Antagonists
antagonists
Antihypertension
Antihypertensive Agents - chemistry
Biphenyl Compounds - chemical synthesis
Biphenyl Compounds - chemistry
Biphenyl Compounds - pharmacology
Drug Design
Humans
Imidazoles - chemical synthesis
Imidazoles - chemistry
Imidazoles - pharmacology
Kinetics
Losartan - chemistry
Models, Molecular
Molecular Conformation
molecular modelling
Molecular Structure
Static Electricity
Stereoisomerism
Structure-Activity Relationship
Tetrazoles - chemical synthesis
Tetrazoles - chemistry
Tetrazoles - pharmacology
Valine - analogs & derivatives
Valine - chemistry
Valsartan
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Summary:Extensive molecular modelling studies, including conformational analysis and the comparison of molecular electrostatic potential distributions, were used to evaluate structural parameters of new antagonists containing acyclic replacements of the N=C-N imidazole region. The synthesis and the biological screening of a series of acyl biphenyltetrazole derivatives were planned and realized to gain an insight into the structure–activity relationships of this unusual class of Angiotensin II antagonists.
ISSN:0968-0896
1464-3391
DOI:10.1016/S0968-0896(98)00160-6