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

We have successfully obtained 1,2,4-oxadiazol-5-one bioisoteres of Am580 or Tazarotene-like retinoids. In particular compound 4 displays an EC50 of 26 nM on RAR-β. We have successfully obtained 1,2,4-oxadiazol-5-one bioisoteres of Am580 or Tazarotene-like retinoids. In particular compound 4 displays...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 19; no. 2; pp. 489 - 492
Main Authors:	Charton, Julie, Deprez-Poulain, Rebecca, Hennuyer, Nathalie, Tailleux, Anne, Staels, Bart, Deprez, Benoit
Format:	Journal Article
Language:	English
Published:	England Elsevier Ltd 15-01-2009 Elsevier
Subjects:	1,2,4-Oxadiazol-5-one Carboxylic Acids - chemistry Life Sciences Oxadiazoles - chemistry Pharmaceutical sciences Receptors, Retinoic Acid - drug effects Retinoid Retinoids - chemistry Retinoids - pharmacology Retinoid 1,2,4-Oxadiazol-5-one
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Summary:	We have successfully obtained 1,2,4-oxadiazol-5-one bioisoteres of Am580 or Tazarotene-like retinoids. In particular compound 4 displays an EC50 of 26 nM on RAR-β. 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 26 nM on RAR-β.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2008.11.040