Novel non-carboxylic acid retinoids: 1,2,4-oxadiazol-5-one derivatives.

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Charton J, Deprez-Poulain R, Hennuyer N, Tailleux A, Staels B, Deprez B

Novel non-carboxylic acid retinoids: 1,2,4-oxadiazol-5-one derivatives.

Bioorg Med Chem Lett. 2009 Jan 15;19(2):489-92. doi: 10.1016/j.bmcl.2008.11.040. Epub 2008 Nov 18.

PubMed ID
19058965 [ View in PubMed
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Abstract

We have successfully obtained 1,2,4-oxadiazol-5-one bioisoteres of Am580 or Tazarotene-like retinoids. In particular compound 4 displays an EC(50) of 26nM on RAR-beta.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
TazaroteneRetinoic acid receptor alphaEC 50 (nM)63N/AN/ADetails
TazaroteneRetinoic acid receptor betaEC 50 (nM)0.8N/AN/ADetails
TazaroteneRetinoic acid receptor gammaEC 50 (nM)40N/AN/ADetails
TretinoinRetinoic acid receptor alphaEC 50 (nM)17N/AN/ADetails
TretinoinRetinoic acid receptor betaEC 50 (nM)12N/AN/ADetails
TretinoinRetinoic acid receptor gammaEC 50 (nM)0.2N/AN/ADetails