title: Selective angiotensin II AT2 receptor agonists: Benzamide structure-activity relationships.
abstract: In the investigation of the structure-activity relationship of nonpeptide AT(2) receptor agonists, a series of substituted benzamide analogues of the selective nonpeptide AT(2) receptor agonist M024 have been synthesised. In a second series, the biphenyl scaffold was compared to the thienylphenyl scaffold and the impact of the isobutyl substituent and its position on AT(1)/AT(2) receptor selectivity was also investigated. Both series included several compounds with high affinity and selectivity for the AT(2) receptor. Three of the compounds were also proven to function as agonists at the AT(2) receptor, as deduced from a neurite outgrowth assay, conducted in NG108-15 cells.
authors.affiliation: Department of Medicinal Chemistry, BMC, Uppsala University, PO Box 574, SE-751 23 Uppsala, Sweden.
authors.forename: Charlotta
authors.initials: C
authors.lastname: Wallinder
authors.forename: Milad
authors.initials: M
authors.lastname: Botros
authors.forename: Ulrika
authors.initials: U
authors.lastname: Rosenström
authors.forename: Marie-Odile
authors.initials: MO
authors.lastname: Guimond
authors.forename: Hélène
authors.initials: H
authors.lastname: Beaudry
authors.forename: Fred
authors.initials: F
authors.lastname: Nyberg
authors.forename: Nicole
authors.initials: N
authors.lastname: Gallo-Payet
authors.forename: Anders
authors.initials: A
authors.lastname: Hallberg
authors.forename: Mathias
authors.initials: M
authors.lastname: Alterman
mesh_terms: D001549:Benzamides / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D006801:Humans; D016501:Neurites / Q000187:drug effects; D044139:Receptor, Angiotensin, Type 2 / Q000819:agonists*; D013329:Structure-Activity Relationship
chemical_list: D001549:Benzamides; D044139:Receptor, Angiotensin, Type 2