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

Sakaki, Junichi and Kishida, Masashi and Konishi, Kazuhide and Gunji, Hiroki and Toyao, Atsushi and Matsumoto, Yuki and Kanazawa, Takanori and Uchiyama, Hidefumi and Fukaya, Hiroaki and Mitani, Hironobu and Arai, Yoshie and Kimura, Masaaki (2007) Synthesis and structure-activity relationship of novel RXR antagonists: orally active anti-diabetic and anti-obesity agents. Bioorganic & Medicinal Chemistry Letters, 17 (17). pp. 4804-4807. ISSN 0960-894X

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.

Item Type: Article
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Additional Information: can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: RXR; Antagonist; Anti-diabetic; Anti-obesity
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Date Deposited: 14 Dec 2009 14:07
Last Modified: 14 Dec 2009 14:07
URI: https://oak.novartis.com/id/eprint/11

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