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Bioorg Med Chem Lett ; 13(3): 379-82, 2003 Feb 10.
Article in English | MEDLINE | ID: mdl-12565933

ABSTRACT

In this communication, we wish to describe the discovery of a novel series of 6-azauracil-based thyromimetics that possess up to 100-fold selectivities for binding and functional activation of the beta(1)-isoform of the thyroid receptor family. Structure-activity relationship studies on the 3,5- and 3'-positions provided compounds with enhanced TR beta affinity and selectivity. Key binding interactions between the 6-azauracil moiety and the receptor have been determined through of X-ray crystallographic analysis.


Subject(s)
Receptors, Thyroid Hormone/drug effects , Thyroid Hormones/pharmacology , Uracil/analogs & derivatives , Uracil/chemistry , Crystallography, X-Ray , Drug Design , Humans , Indicators and Reagents , Ligands , Models, Molecular , Molecular Mimicry , Protein Binding , Protein Conformation , Structure-Activity Relationship , Uracil/pharmacology
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