Thiazolidinediones with thyroid hormone receptor agonistic activity.
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.
Ebisawa
M
M
Graduate School of Pharmaceutical Sciences, University of Tokyo, Japan.
Inoue
N
N
Fukasawa
H
H
Sotome
T
T
Kagechika
H
H
D000818:Animals; D019556:COS Cells; D006801:Humans; D008156:Luciferases / Q000235:genetics / Q000378:metabolism; D009687:Nuclear Proteins / Q000378:metabolism; D018160:Receptors, Cytoplasmic and Nuclear / Q000378:metabolism; D018168:Receptors, Retinoic Acid / Q000187:drug effects; D011988:Receptors, Thyroid Hormone / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D014157:Transcription Factors / Q000378:metabolism
D009687:Nuclear Proteins; D018160:Receptors, Cytoplasmic and Nuclear; D018168:Receptors, Retinoic Acid; D011988:Receptors, Thyroid Hormone; D013844:Thiazoles; D014157:Transcription Factors; D008156:Luciferases