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Synthesis and structure-activity relationship of novel RXR antagonists: orally active anti-diabetic and anti-obesity agents |
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| Authors: | Sakaki Junichi Kishida Masashi Konishi Kazuhide Gunji Hiroki Toyao Atsushi Matsumoto Yuki Kanazawa Takanori Uchiyama Hidefumi Fukaya Hiroaki Mitani Hironobu Arai Yoshie Kimura Masaaki |
| Institution: | Novartis Institute for Biomedical Research, Tsukuba Research Institute, Ohkubo 8, Tsukuba-Shi, Ibaraki, Japan. |
| Abstract: | A series of diazepinylbenzoic acid derivatives were synthesized and tested in the inhibition assay of the transactivation of RXR. Oral treatment of cyano derivatives (16f) was found to show anti-diabetic and anti-obesity effects in KK-A(y) mice. |
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