title: Synthesis and pharmacological evaluation of a new class of peroxisome proliferator-activated receptor modulators.
abstract: A series of 5-substituted 2-benzoylaminobenzoic acids has been synthesized and assayed for PPARalpha/gamma activity. Both dual activators and selective PPARgamma agonists have been identified. This class of compounds was shown to activate the PPARgamma receptor through interaction with a novel binding site.
authors.affiliation: Biovitrum AB, Department of Medicinal Chemistry, Rapsgatan 7, Uppsala 751-37, Stockholm, Sweden. markus.thor@biovitrum.com
authors.forename: Markus
authors.initials: M
authors.lastname: Thor
authors.forename: Katarina
authors.initials: K
authors.lastname: Beierlein
authors.forename: Graeme
authors.initials: G
authors.lastname: Dykes
authors.forename: Anna Lena
authors.initials: AL
authors.lastname: Gustavsson
authors.forename: Jessica
authors.initials: J
authors.lastname: Heidrich
authors.forename: Lena
authors.initials: L
authors.lastname: Jendeberg
authors.forename: Bengt
authors.initials: B
authors.lastname: Lindqvist
authors.forename: Cecile
authors.initials: C
authors.lastname: Pegurier
authors.forename: Patrick
authors.initials: P
authors.lastname: Roussel
authors.forename: Martin
authors.initials: M
authors.lastname: Slater
authors.forename: Stefan
authors.initials: S
authors.lastname: Svensson
authors.forename: Mona
authors.initials: M
authors.lastname: Sydow-Bäckman
authors.forename: Ulla
authors.initials: U
authors.lastname: Thornström
authors.forename: Jonas
authors.initials: J
authors.lastname: Uppenberg
mesh_terms: D062365:Aminobenzoates / Q000138:chemical synthesis* / Q000494:pharmacology*; D001665:Binding Sites; D018360:Crystallography, X-Ray; D006801:Humans; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists* / Q000235:genetics; D013329:Structure-Activity Relationship; D014157:Transcription Factors / Q000819:agonists* / Q000235:genetics; D015533:Transcriptional Activation / Q000187:drug effects; D014162:Transfection; D014407:Tumor Cells, Cultured
chemical_list: D062365:Aminobenzoates; D018160:Receptors, Cytoplasmic and Nuclear; D014157:Transcription Factors