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Novel selective PPARdelta agonists: optimization of activity by modification of alkynylallylic moiety
M Havranek, P Sauerberg, JP Mogensen, P Kratina, CB Jeppesen, I Pettersson, P Pihera
Bioorganic & medicinal chemistry letters.
2007 ;
17 (15) :
4144-4149.
Jazyk angličtina Země Velká Británie
Perzistentní odkaz
https://www.medvik.cz/link/bmc10010219
Online
NLK
ScienceDirect (archiv)
od 1993-01-01 do 2009-12-31
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.
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