Synthesis and pharmacological evaluation of a new class of peroxisome proliferator-activated receptor modulators.
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.
Thor
Markus
M
Biovitrum AB, Department of Medicinal Chemistry, Rapsgatan 7, Uppsala 751-37, Stockholm, Sweden. markus.thor@biovitrum.com
Beierlein
Katarina
K
Dykes
Graeme
G
Gustavsson
Anna Lena
AL
Heidrich
Jessica
J
Jendeberg
Lena
L
Lindqvist
Bengt
B
Pegurier
Cecile
C
Roussel
Patrick
P
Slater
Martin
M
Svensson
Stefan
S
Sydow-Bäckman
Mona
M
Thornström
Ulla
U
Uppenberg
Jonas
J
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
D062365:Aminobenzoates; D018160:Receptors, Cytoplasmic and Nuclear; D014157:Transcription Factors