【文章名】Peroxisome proliferator-activated receptor (PPAR) agonists with 3,4-dihydro-2H-benzo[e][1,3]oxazine and 2,3,4,5-tetrahydrobenzo[f][1,4]oxazepine skeletons: effects of cyclization of linker moiety on PPAR-agonistic activity.
Peroxisome proliferator-activated receptor (PPAR) agonists with 3,4-dihydro-2H-benzo[e][1,3]oxazine and 2,3,4,5-tetrahydrobenzo[f][1,4]oxazepine skeletons: effects of cyclization of linker moiety on PPAR-agonistic activity.
[摘要]：Conformationally restricted heterocyclic derivs. of KCL ((S)-2-{4-methoxy-3-[4-(trifluoromethyl)benzylcarbamoyl]benzyl}butanoic acid), which exhibit selective PPARa-agonistic activity, were prepd. to examine the significance of the amide bond of KCL. In vitro transactivation assay clearly indicated that introduction of a 2-position fluorine atom enhanced PPARs-agonistic activity as expected, while cyclization of the amide bond caused a drastic decrease of PPARs-agonistic activity.
