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Communication | Regular issue | Vol 78, No. 9, 2009, pp.2209-2216
Published online, 29th May, 2009
DOI: 10.3987/COM-09-11738
Liver X Receptor (LXR) Modulators with Dibenz[b,f][1,4]oxazepin-11-one, (Z)-Dibenz[b,f]azocin-6-one, and 11,12-Dihydrodibenz[b,f]azocin-6-one Skeletons

Atsushi Aoyama, Hiroshi Aoyama, Makoto Makishima, Yuichi Hashimoto, and Hiroyuki Miyachi*

*Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University, 1-1-1 Tsushima-naka, Okayama 700-8530, Japan

Abstract

Conformationally restricted heterocyclic analogs of carba-T0901317 with dibenz[b,f][1,4]oxazepin-11-one, 11,12-dihydrodibenz[b,f]azocin-6-one, and (Z)-dibenz[b,f]-azocin-6-one skeletons were prepared as candidate for liver X receptor (LXR) agonists. In vitro transactivation assay revealed that the activity depends on the nature of the linking group.