Novel heterocyclic thyromimetics. Part 2.

Haning H ¹,

Mueller U ,

Schmidt G ,

Schmeck C ,

Voehringer V ,

Kretschmer A ,

Bischoff H

Affiliations

1. Bayer HealthCare AG, Bayer Schering Pharma Global Drug Discovery, D-42096 Wuppertal, Germany.
Authors
Haning H¹
(1 author)

Bioorganic & Medicinal Chemistry Letters, 29 Apr 2007, 17(14):3992-3996
https://doi.org/10.1016/j.bmcl.2007.04.085 PMID: 17499989

Abstract

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.

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References

Articles referenced by this article (26)

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Small molecules (chemicals) in ChEMBL (Showing 10 of 22)

5-(4-(4-hydroxy-3-isopropylphenoxy)-3,5-diisopropylbenzyl)thiazolidine-2,4-dione(CHEMBL - CHEMBL245462)
Thyroid hormone receptor(CHEMBL - CHEMBL2111462)
4,6-dibromo-5-(3-isopropyl-4-methoxyphenoxy)benzofuran-2-carboxylic acid(CHEMBL - CHEMBL245508)
4,6-dibromo-5-(3-(4-fluorobenzoyl)-4-hydroxyphenoxy)benzofuran-2-carboxylic acid(CHEMBL - CHEMBL247912)
4,6-dibromo-5-(3-((4-fluorophenyl)(hydroxy)methyl)-4-hydroxyphenoxy)benzofuran-2-carboxylic acid(CHEMBL - CHEMBL247913)
5-(4-(4-hydroxy-3-isopropylphenoxy)-3,5-dimethylbenzyl)thiazolidine-2,4-dione(CHEMBL - CHEMBL248111)
5-(4-hydroxy-3-isopropylphenoxy)-4,6-dimethylbenzofuran-2-carboxylic acid(CHEMBL - CHEMBL248314)
2-(5-(4-hydroxy-3-isopropylphenoxy)-4,6-dimethyl-2,3-dihydrobenzofuran-2-yl)acetic acid(CHEMBL - CHEMBL248315)
2-(6-(4-hydroxy-3-isopropylphenoxy)-5,7-dimethylbenzofuran-3-yl)acetic acid(CHEMBL - CHEMBL248515)
Mus musculus(CHEMBL - CHEMBL375)

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Novel heterocyclic thyromimetics. Part 2.

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Abstract

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