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Synthesis and biological evaluation of novel (-)-Cercosporamide derivatives as potent selective PPARγ modulators. 2012
Akihiro Furukawa, and
Tsuyoshi Arita, and
Takehiro Fukuzaki, and
Makoto Mori, and
Takeshi Honda, and
Susumu Satoh, and
Yumi Matsui, and
Kenji Wakabayashi, and
Shinko Hayashi, and
Kouichi Nakamura, and
Kazushi Araki, and
Masanori Kuroha, and
Jun Tanaka, and
Satoko Wakimoto, and
Osamu Suzuki, and
Jun Ohsumi
Shinagawa R&D Center, Daiichi Sankyo Co., Ltd., 1-2-58, Hiromachi, Tokyo 140 8710, Japan. furukawa.akihiro.zy@daiichisankyo.co.jp
Selective peroxisome proliferator-activated receptor gamma (PPARγ) modulators are expected to be a novel class of drugs improving plasma glucose levels without PPARγ-related adverse effects. As a continuation of our studies for (-)-Cercosporamide derivatives as selective PPARγ modulators, we synthesized substituted naphthalene type compounds and identified the most potent compound 15 (EC(50) = 0.94 nM, E(max) = 38%). Compound 15 selectively activated PPARγ transcription and did not activate PPARα and PPARδ. The potassium salt of compound 15 showed a high solubility and a good oral bioavailability (58%). Oral administration of the potassium salt remarkably improved the plasma glucose levels of female Zucker diabetic fatty rats at 1 mg/kg. Moreover, it did not cause a plasma volume increase or a cardiac enlargement in Wistar-Imamichi rats, even at 100 mg/kg.
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