Novel heterocyclic thyromimetics. Part 2.
Novel heterocyclic thyromimetics are presented carrying carboxy-substituted benzofurans or sulfur containing heterocycles, as replacements for the amino acid side chain of T3. Potent agonists were identified in both series. SAR trends are examined and found to be mostly consistent with previously published thyromimetics. The lack of isoform selectivity demonstrated with isoform-selective transient THR transfection assays has been confirmed by corresponding in vivo studies.
Haning
Helmut
H
Bayer HealthCare AG, Bayer Schering Pharma Global Drug Discovery, D-42096 Wuppertal, Germany. Helmut.Haning@bayerhealthcare.com
Mueller
Ulrich
U
Schmidt
Gunter
G
Schmeck
Carsten
C
Voehringer
Verena
V
Kretschmer
Axel
A
Bischoff
Hilmar
H
D006571:Heterocyclic Compounds / Q000494:pharmacology*; D018716:Molecular Mimicry; D013329:Structure-Activity Relationship; D013963:Thyroid Hormones / Q000494:pharmacology*
D006571:Heterocyclic Compounds; D013963:Thyroid Hormones