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

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-Ay 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-Ay mice.Figure optionsDownload as PowerPoint slide