Abstract
Several thiazolidinedione derivatives (3-7) were designed and synthesized as candidate thyromimetic drugs. Among them, the dihydrogenated compounds, such as 5-2-[[4-(3-tert-butyl-4-hydroxyphenyl)oxy-3,5-diiodophenyl] ethyl]-2,4-thiazolidinedione (6b) and its 3-isopropyl analog (7b), exhibited potent thyroid hormone receptor alpha 1 (TR alpha 1) activation activity.
MeSH terms
-
Animals
-
COS Cells
-
Humans
-
Luciferases / genetics
-
Luciferases / metabolism
-
Nuclear Proteins / metabolism
-
Receptors, Cytoplasmic and Nuclear / metabolism
-
Receptors, Retinoic Acid / drug effects
-
Receptors, Thyroid Hormone / antagonists & inhibitors*
-
Structure-Activity Relationship
-
Thiazoles / chemical synthesis*
-
Thiazoles / pharmacology
-
Transcription Factors / metabolism
Substances
-
Nuclear Proteins
-
Receptors, Cytoplasmic and Nuclear
-
Receptors, Retinoic Acid
-
Receptors, Thyroid Hormone
-
Thiazoles
-
Transcription Factors
-
Luciferases