title: Synthesis and structure-activity relationship of novel RXR antagonists: orally active anti-diabetic and anti-obesity agents.
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.
authors.affiliation: Novartis Institute for Biomedical Research, Tsukuba Research Institute, Ohkubo 8, Tsukuba-Shi, Ibaraki, Japan.
authors.forename: Junichi
authors.initials: J
authors.lastname: Sakaki
authors.forename: Masashi
authors.initials: M
authors.lastname: Kishida
authors.forename: Kazuhide
authors.initials: K
authors.lastname: Konishi
authors.forename: Hiroki
authors.initials: H
authors.lastname: Gunji
authors.forename: Atsushi
authors.initials: A
authors.lastname: Toyao
authors.forename: Yuki
authors.initials: Y
authors.lastname: Matsumoto
authors.forename: Takanori
authors.initials: T
authors.lastname: Kanazawa
authors.forename: Hidefumi
authors.initials: H
authors.lastname: Uchiyama
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Fukaya
authors.forename: Hironobu
authors.initials: H
authors.lastname: Mitani
authors.forename: Yoshie
authors.initials: Y
authors.lastname: Arai
authors.forename: Masaaki
authors.initials: M
authors.lastname: Kimura
mesh_terms: D000818:Animals; D019440:Anti-Obesity Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001835:Body Weight; D004041:Dietary Fats; D015195:Drug Design; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D008297:Male; D051379:Mice; D008822:Mice, Transgenic; D008956:Models, Chemical; D047490:Retinoid X Receptor alpha / Q000037:antagonists & inhibitors* / Q000138:chemical synthesis* / Q000737:chemistry*; D013329:Structure-Activity Relationship; D015533:Transcriptional Activation
chemical_list: D019440:Anti-Obesity Agents; D004041:Dietary Fats; D007004:Hypoglycemic Agents; D047490:Retinoid X Receptor alpha