Synthesis and structure–activity relationship of novel RXR antagonists: Orally active anti-diabetic and anti-obesity agents

J Sakaki, M Kishida, K Konishi, H Gunji, A Toyao…

Index: Sakaki, Junichi; Kishida, Masashi; Konishi, Kazuhide; Gunji, Hiroki; Toyao, Atsushi; Matsumoto, Yuki; Kanazawa, Takanori; Uchiyama, Hidefumi; Fukaya, Hiroaki; Mitani, Hironobu; Arai, Yoshie; Kimura, Masaaki Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 17 p. 4804 - 4807

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Citation Number: 21

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. ... A series of diazepinylbenzoic acid derivatives were synthesized and tested in the inhibition assayof the transactivation of RXR. Oral treatment of cyano derivatives showed anti-diabetic and anti-obesity effects in KK-A y mice.