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Communication | Regular issue | Vol 75, No. 9, 2008, pp.2187-2192
Published online, 15th May, 2008
DOI: 10.3987/COM-08-11407
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

Kenji Ohgane, Jyun-ichi Kasuga, Takuji Ohyama, Yuko Hirakawa, Kosuke Morikawa, Makoto Makishima, Yuichi Hashimoto, and Hiroyuki Miyachi*

*Institute of Molecular and Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan

Abstract

Conformationally restricted heterocyclic derivatives of KCL ((S)-2-{4-methoxy-3-[4-(trifluoromethyl)benzylcarbamoyl]benzyl}butanoic acid), which exhibit selective PPAR±-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.