Probucol

Probucol is an anti-hyperlipidemic drug by lowering the level of cholesterol in the bloodstream by increasing the rate of LDL catabolism.Target: OthersProbucol is a drug used to lower LDL and HDL cholesterol yet has little effect on serum-triglyceride or VLDL cholesterol. Probucol inhibited cholesterol efflux up to 80% in J774 macrophages expressing ABCA1. probucol is an effective inhibitor of ABCA1-mediated cholesterol efflux without influencing scavenger receptor class B type I-mediate

Solid

Probucol is a dithioketal that is propane-2,2-dithiol in which the hydrogens attached to both sulfur atoms are replaced by 3,5-di-tert-butyl-4-hydroxyphenyl groups. An anticholesteremic drug with antioxidant and anti-inflammatory properties, it is used to treat high levels of cholesterol in blood. It has a role as an anticholesteremic drug, an antioxidant, an anti-inflammatory drug, a cardiovascular drug and an antilipemic drug. It is a dithioketal and a polyphenol.|A drug used to lower LDL and HDL cholesterol yet has little effect on serum-triglyceride or VLDL cholesterol. (From Martindale, The Extra Pharmacopoeia, 30th ed, p993).|Probucol is a bis-phenol antioxidant with antilipidemic activity. Probucol inhibits oxidation of low density lipoprotein and lowers the level of cholesterol in the bloodstream by increasing the rate of LDL catabolism.

To 2, 6-di-tert-butyl-4-mercaptophenol (100 g) produced in Example 4 was added methanol (170 ml) and water (10 g) and the mixture was heated at 50 to 55°C. Acetone (29.2 g) was added to this, and 35percent hydrochloric acid (4 g) was dropped into the mixture which was reacted for 5 hours at the same temperature. The fact that the amount of raw materials reached 5percent or less was confirmed by the HPLC method, then, the mixture was cooled to 0 to 5°C , and aged for about 3 hours at the same temperature. The mixture was filtrated, and the crystal was washed with 80percent isopropanol (25.7 ml). The wet crystal (123.3 g) was dissolved in 218 ml of isopropanol with heating, and the solution was filtrated, then, the filtration apparatus and the like used were washed with isopropanol (17.3 ml). The filtrate and washing liquid were combined, and once heated and complete dissolution thereof was confirmed, then, the solution was cooled and aged at 0 to 5°C. The crystal was filtrated, washed with isopropanol (30 ml), and dried to obtain a crystal (88.74 g) of 4, 4'-isopropylidenedithiobis[2, 6-di-tert-butylphenol]. The yield of 82percent and the purity was 99.9percent.

An antioxidant, anti-inflammatory, and hypocholesterolemic agent which inhibits atherogenesis in murine models.

Molecular Weight:516.8
XLogP3:11.3
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:4
Rotatable Bond Count:8
Exact Mass:516.30957312
Monoisotopic Mass:516.30957312
Topological Polar Surface Area:91.1
Heavy Atom Count:35
Complexity:583
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes