title: Novel selective PPARdelta agonists: optimization of activity by modification of alkynylallylic moiety.
abstract: Y-shaped molecules bearing alkynylallylic moieties were found to be potent and selective PPARdelta activators. The alkynylallylic moiety was synthesized from alkyn-1-ols by hydroalumination followed by a cross-coupling reaction. Series of active compounds 6 were obtained by stepwise changing the structure of the known PPARpan agonist 5 into Y-shaped compounds. The most active and selective compound, 6f, had a PPARdelta potency of 0.13 microM, which is 50-fold more potent than compound 5.
authors.affiliation: RE&D VUFB, s.r.o., Podebradská 56/186, 180 66 Praha 9, Czech Republic. havranek@readvufb.cz
authors.forename: Miroslav
authors.initials: M
authors.lastname: Havranek
authors.forename: Per
authors.initials: P
authors.lastname: Sauerberg
authors.forename: John P
authors.initials: JP
authors.lastname: Mogensen
authors.forename: Pavel
authors.initials: P
authors.lastname: Kratina
authors.forename: Claus B
authors.initials: CB
authors.lastname: Jeppesen
authors.forename: Ingrid
authors.initials: I
authors.lastname: Pettersson
authors.forename: Pavel
authors.initials: P
authors.lastname: Pihera
mesh_terms: D008958:Models, Molecular; D015394:Molecular Structure; D047494:PPAR delta / Q000819:agonists*
chemical_list: D047494:PPAR delta