1078725-45-7Relevant articles and documents
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
Ohgane, Kenji,Kasuga, Jyun-Ichi,Ohyama, Takuji,Hirakawa, Yuko,Morikawa, Kosuke,Makishima, Makoto,Hashimoto, Yuichi,Miyachi, Hiroyuki
, p. 2187 - 2192 (2011/04/18)
Conformationally restricted heterocyclic derivatives of KCL ((S)-2-{4-methoxy-3-[4-(trifluoromethyl)benzylcarbamoyl]benzyl}butanoic acid), which exhibit selective PPARα-agonistic activity, were prepared 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. The Japan Institute of Heterocyclic Chemistry.