Novel thyroid hormone receptor antagonists with an N-alkylated diphenylamine skeleton

Thyroid hormones play important roles in growth, development and homeostasis, and disruption of their functions induces serious disease, so novel synthetic thyroid hormone analogues are candidates for clinical application. We designed and synthesized novel diphenylamine derivatives with a thiazolidinedione moiety as the terminal polar group as thyroid hormone receptor (TR) antagonists. Compounds bearing an appropriately sized N-alkyl group showed antagonistic activities towards both the hTRα1 and hTRβ1 subtypes.

Novel diphenylamine derivatives containing a thiazolidinedione moiety were designed and synthesized, and their antagonistic activities towards the thyroid hormone receptor (TR) subtypes TRα and TRβ were evaluated.Figure optionsDownload as PowerPoint slide