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 EC(50) of 26nM on RAR-beta.
Charton
Julie
J
INSERM U761 Biostructures and Drug Discovery, 3 rue du Professeur Laguesse, Lille F-59006, France. julie.charton@univ-lille2.fr
Deprez-Poulain
Rebecca
R
Hennuyer
Nathalie
N
Tailleux
Anne
A
Staels
Bart
B
Deprez
Benoit
B
D002264:Carboxylic Acids / Q000737:chemistry*; D010069:Oxadiazoles / Q000737:chemistry*; D018168:Receptors, Retinoic Acid / Q000187:drug effects; D012176:Retinoids / Q000737:chemistry / Q000494:pharmacology*
D002264:Carboxylic Acids; D010069:Oxadiazoles; D018168:Receptors, Retinoic Acid; D012176:Retinoids; C082925:retinoic acid receptor beta