443924-70-7Relevant articles and documents
Synthesis and antiplatelet activity of gemfibrozil chiral analogues
Ammazzalorso, Alessandra,Amoroso, Rosa,Baraldi, Mario,Bettoni, Giancarlo,Braghiroli, Daniela,De Filippis, Barbara,Duranti, Andrea,Moretti, Marco,Tortorella, Paolo,Tricca, Maria Luisa,Vezzalini, Francesca
, p. 817 - 821 (2002)
The chiral analogues of gemfibrozil 5-(2,5-dimethylphenoxy)-2-methylpentanoic acid and 5-(2,5-dimethylphenoxy)-2-ethylpentanoic acid were synthesized in optically active form using (S)-4-(1-methylethyl)-2-oxazolidinone as chiral auxiliary. All compounds inhibit human platelet aggregation. From these data, one can surmise that all tested compounds and gemfibrozil act at the platelet level with different mechanism than that of ASA, even if with a different potency.
Synthesis and biological evaluation of novel SIPI-7623 derivatives as farnesoid X receptor (FXR) antagonists
Nian, Si-Yun,Wang, Guo-Ping,Jiang, Zheng-Li,Xiao, Ying,Huang, Mo-Han,Zhou, Yi-Huan,Tan, Xiang-Duan
, p. 1 - 15 (2018/07/13)
Most of reported steroidal FXR antagonists are restricted due to low potency. We described the design and synthesis of novel nonsteroidal scaffold SIPI-7623 derivatives as FXR antagonists. The most potent compound A-11 (IC50 = 7.8 ± 1.1 μM) showed better activity compared to SIPI-7623 (IC50 = 40.8 ± 1.7 μM) and guggulsterone (IC50 = 45.9 ± 1.1 μM). Docking of A-11 in FXR’s ligand-binding domain was also studied.
