title: Design and synthesis of nonpeptide angiotensin II receptor antagonists featuring acyclic imidazole-mimicking structural units.
abstract: Extensive molecular modelling studies, including conformational analysis and the comparison of molecular electrostatic potential distributions, wee 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.
authors.affiliation: University of Milano, Organic and Industrial Chemistry Department, C.N.R. Centre for the Study of Organic and Natural Compounds, Italy.
authors.forename: M
authors.initials: M
authors.lastname: Angiolini
authors.forename: L
authors.initials: L
authors.lastname: Belvisi
authors.forename: D
authors.initials: D
authors.lastname: Poma
authors.forename: A
authors.initials: A
authors.lastname: Salimbeni
authors.forename: N
authors.initials: N
authors.lastname: Sciammetta
authors.forename: C
authors.initials: C
authors.lastname: Scolastico
mesh_terms: D057911:Angiotensin Receptor Antagonists; D000959:Antihypertensive Agents / Q000737:chemistry; D001713:Biphenyl Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D015195:Drug Design; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D007700:Kinetics; D019808:Losartan / Q000737:chemistry; D008958:Models, Molecular; D008968:Molecular Conformation; D015394:Molecular Structure; D055672:Static Electricity; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013777:Tetrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D014633:Valine / Q000031:analogs & derivatives / Q000737:chemistry; D000068756:Valsartan
chemical_list: D057911:Angiotensin Receptor Antagonists; D000959:Antihypertensive Agents; D001713:Biphenyl Compounds; D007093:Imidazoles; D013777:Tetrazoles; D000068756:Valsartan; D014633:Valine; D019808:Losartan