- Tuning Nuclear Receptor Selectivity of Wy14,643 towards Selective Retinoid X Receptor Modulation
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The fatty acid sensing nuclear receptor families retinoid X receptors (RXRs) and peroxisome proliferator-activated receptors (PPARs) hold therapeutic potential in neurodegeneration. Valuable pleiotropic activities of Wy14,643 in models of such conditions
- Pollinger, Julius,Gellrich, Leonie,Schierle, Simone,Kilu, Whitney,Schmidt, Jurema,Kalinowsky, Lena,Ohrndorf, Julia,Kaiser, Astrid,Heering, Jan,Proschak, Ewgenij,Merk, Daniel
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p. 2112 - 2126
(2019/03/08)
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- Pyrimidine and s-triazine derivatives with antilipidemic activity
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Pyrimidine and s-triazine derivatives of formula (I) (I) in which X=CH or N; Y=for example halogen, alkoxy; W=for example -S-CH2-COOH, -O-CH2-COO alkyl, -NH-CH2-CONHCH2CH2OH; Z=for example 2,3-xylidino, and methods for the preparation thereof are described. The compounds show high antilipemic activity.
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- Novel pyrimidine and 1,3,5-triazine hypolipidemic agents
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New compounds were synthesized by changing the substituents of a trisubstituted pyrimidine, i.e., [[4-chloro-6-[(2,3-dimethylphenyl)amino]-2-pyrimidinyl]thio]acetic acid, a potent hypolipidemic agent, impaired, however, by a marked hepatomegaly-inducing effect. The structural variations led to the subsidence (14b, i.e., 4-chloro-2-(dimethylamino)-6-[(2,3-dimethylphenyl)amino]pyrimidine) or to the reduction (18b, [[4-chloro-6-[(2,3-dimethylphenyl)amino]-2-pyrimidinyl]amino]acetic acid) of said untoward effect but still maintained the hypolipidemic effect that, although markedly decreased, still proves significant for serum cholesterol and triglycerides (18b) or for serum triglycerides only (14b).
- d'Atri,Gomarasca,Resnati,Tronconi,Scolastico,Sirtori
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p. 1621 - 1629
(2007/10/02)
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