Sauerberg, Per published the artcileIdentification and Synthesis of a Novel Selective Partial PPARδ Agonist with Full Efficacy on Lipid Metabolism In Vitro and In Vivo, Application of 3-Chloro-4-hydroxyphenylacetic acid, the publication is Journal of Medicinal Chemistry (2007), 50(7), 1495-1503, database is CAplus and MEDLINE.
The aim was to identify a novel selective PPARδ agonist with full efficacy on free fatty acid (FFA) oxidation in vitro and plasma lipid correction in vivo. Using the triple PPARα,γ,δ agonist 1 (I) as the structural starting point, we wanted to investigate the possibility of obtaining selective PPARδ agonists by modifying only the acidic part of 1, while holding the lipophilic half of the mol. constant The structure-activity relationship was guided by in vitro transactivation data using the human PPAR receptors, FFA oxidation efficacy performed in the rat muscle L6 cell line, and in vivo rat pharmacokinetic properties. Compound 7 ([4-[3,3-bis-(4-bromo-phenyl)-allylthio]-2-chloro-phenoxy]-acetic acid) was identified as a selective, partial agonist with good oral pharmacokinetic properties in rat. Chronic treatment of high fat fed ApoB100/CETP-Tgn mice with 7 corrected the plasma lipid parameters and improved insulin sensitivity. These data suggest that selective PPARδ agonists have the potential to become a novel treatment of dyslipidemia.
Journal of Medicinal Chemistry published new progress about 33697-81-3. 33697-81-3 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene,Phenol, name is 3-Chloro-4-hydroxyphenylacetic acid, and the molecular formula is C8H7ClO3, Application of 3-Chloro-4-hydroxyphenylacetic acid.
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