title: The conformation and activity relationship of fused analogs of DuP753.
abstract: We have prepared three conformationally restricted analogs of DuP753 in which one of the phenyl rings in the biphenyl moiety is fused to the imidazole ring, and have investigated the conformation-biological activity relationship of these compounds. Conformational analysis on DuP753 and these compounds confirms that a specific 3-dimensional arrangement of pharmacophoric elements is essential for biological activity.
authors.affiliation: Korea Research Institute of Chemical Technology, Dae-Jeon.
authors.forename: S E
authors.initials: SE
authors.lastname: Yoo
authors.forename: Y A
authors.initials: YA
authors.lastname: Shin
authors.forename: S H
authors.initials: SH
authors.lastname: Lee
authors.forename: N J
authors.initials: NJ
authors.lastname: Kim
mesh_terms: D000804:Angiotensin II / Q000378:metabolism; D057911:Angiotensin Receptor Antagonists; D000818:Animals; D001713:Biphenyl Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D019808:Losartan; D008862:Microsomes, Liver / Q000737:chemistry; D008958:Models, Molecular; D008968:Molecular Conformation; D015394:Molecular Structure; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship; D013777:Tetrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D057911:Angiotensin Receptor Antagonists; D001713:Biphenyl Compounds; D007093:Imidazoles; D013777:Tetrazoles; D000804:Angiotensin II; D019808:Losartan