title: Nonpeptide angiotensin II receptor antagonists: N-[(benzyloxy)benzyl]imidazoles and related compounds as potent antihypertensives.
abstract: A series of compounds has been synthesized and demonstrated to be antagonists of the angiotensin II (AII) receptor. These compounds are structurally related to the N-(benzamidobenzyl)imidazoles and extend the scope of this new class of nonpeptide AII antagonists. It has been found that the amide linkage (X = NHCO) in the N-(benzamidobenzyl)imidazoles can be replaced successfully by a variety of groups (X = single bond, O, S, CO, OCH2, CH = CH, NHCONH); linkers of 0-1 atoms in length are most effective. When administered intravenously to awake renal hypertensive rats, these compounds are potent antihypertensives.
authors.affiliation: Medicinal Chemistry Section, E. I. du Pont de Nemours and Co., Inc., Wilmington, Delaware 19880.
authors.forename: D J
authors.initials: DJ
authors.lastname: Carini
authors.forename: J V
authors.initials: JV
authors.lastname: Duncia
authors.forename: A L
authors.initials: AL
authors.lastname: Johnson
authors.forename: A T
authors.initials: AT
authors.lastname: Chiu
authors.forename: W A
authors.initials: WA
authors.lastname: Price
authors.forename: P C
authors.initials: PC
authors.lastname: Wong
authors.forename: P B
authors.initials: PB
authors.lastname: Timmermans
mesh_terms: D000302:Adrenal Cortex / Q000187:drug effects / Q000378:metabolism; D000804:Angiotensin II / Q000037:antagonists & inhibitors*; D057911:Angiotensin Receptor Antagonists; D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis*; D001667:Binding, Competitive; D055598:Chemical Phenomena; D002621:Chemistry; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D008861:Microsomes / Q000187:drug effects / Q000378:metabolism; D051381:Rats; D011945:Receptors, Angiotensin / Q000187:drug effects* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D057911:Angiotensin Receptor Antagonists; D000959:Antihypertensive Agents; D007093:Imidazoles; D011945:Receptors, Angiotensin; D000804:Angiotensin II