Novel 3,5-diaryl pyrazolines and pyrazole as low-density lipoprotein (LDL) oxidation inhibitor.
Compounds 4a-j and 5 were synthesized by cyclocondensation of 3a-j and hydrazine and showed significant LDL-antioxidant activities in the TBARS assay, the lag time of conjugated diene production, the relative electrophoretic mobility (REM) of ox-LDL, the apoB-100 fragmentation, and the macrophage-mediated LDL oxidation. Among compounds 4a-j and 5, 4a was found to be the most active compound as an inhibitor of LDL oxidation and 4a (IC50 = 0.1 microM) was 6-fold more potent than probucol (IC50 = 0.6 microM) in the TBARS assay.
Jeong
Tae-Sook
TS
National Research Laboratory of Lipid Metabolism & Atherosclerosis, Korea Research Institute of Bioscience and Biotechnology, Daejeon 305-333, South Korea.
Kim
Kyung Soon
KS
Kim
Ju-Ryoung
JR
Cho
Kyung-Hyun
KH
Lee
Sangku
S
Lee
Woo Song
WS
D000975:Antioxidants / Q000138:chemical synthesis* / Q000494:pharmacology; D003300:Copper / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D015227:Lipid Peroxidation / Q000187:drug effects; D008077:Lipoproteins, LDL / Q000037:antagonists & inhibitors / Q000187:drug effects* / Q000378:metabolism; D008264:Macrophages / Q000378:metabolism; D010084:Oxidation-Reduction; D011720:Pyrazoles / Q000138:chemical synthesis / Q000494:pharmacology*; D017392:Thiobarbituric Acid Reactive Substances
D000975:Antioxidants; D008077:Lipoproteins, LDL; D011720:Pyrazoles; D017392:Thiobarbituric Acid Reactive Substances; C099252:oxidized low density lipoprotein; D003300:Copper