Antihyperlipidemic morpholine derivatives with antioxidant activity: An investigation of the aromatic substitution

Discovery of Potential Inhibitors of Squalene Synthase from Traditional Chinese Medicine Based on Virtual Screening and In Vitro Evaluation of Lipid-Lowering Effect

“…D99 and TAK-475 both formed hydrophobic interactions with PHE54, VAL179, LEU183, LEU211, and PRO292. Thus, these amino acids were regarded as key residues, which is consistent with the literature [ 25 , 26 ].…”

“…Tavridou et al [ 61 ] demonstrated that SQS inhibitors could significantly reduce the TG level in HepG2 cells. Moreover, other related literature has indicated that SQS inhibitors can decrease the TG level in in vivo experiments [ 26 , 62 ]. To measure the lipidemic parameter triglyceride (TG) level, appropriate kits were utilized to analyze the TG content in HepG2 cells.…”

Morpholine as a privileged structure: A review on the medicinal chemistry and pharmacological activity of morpholine containing bioactive molecules

“…Docking studies of the active site of SQS with several of these compounds revealed the formation of an H‐bond of the hemiaketalic OH with Asp80 and lipophilic interactions of the aromatic moiety with the large lipophilic cavity in the active site of the enzyme, rendering those structural components critical for SQS inhibition . In this case, morpholine serves as a useful structural scaffold for supporting further variable substitution as shown in subsequent studies; based on structure 37 , a further modification involved the incorporation of a stilbene moiety, resulting in the general structure 38 shown in Figure .…”

Novel Pyrimidine‐based Ferrocenyl substituted Organometallic Compounds: Synthesis, Characterization and Biological Evaluation

“…Also, a number of reports have been suggested the potential of morpholine derivatives as effective anticancer agents . Beside this, morpholine containing compounds also have been reported to exhibit diverse biological properties such as γ‐secretase inhibitors, antioxidant and anti‐inflammatory . According to mechanism of action of morpholine derivatives it is clear, that these derivatives prevent the biosynthesis of sterol by blocking two successive enzymatic processes: (1) inhibiting the biotransformation of lanosterol into zymosterol by blocking the enzyme C‐14 sterol reductase and; (2) inhibiting the synthesis of ergosterol from the biotransformation of fecosterol into episterol by blocking the enzyme C‐8 sterol isomerase .…”