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 (IC 50=0.1μM) was 6-fold more potent than probucol (IC 50=0.6μM) in the TBARS assay.
Jeong, Tae-Sook,Kim, Kyung Soon,Kim, Ju-Ryoung,Cho, Kyung-Hyun,Lee, Sangku,Lee, Woo Song
Novel 3,5-diaryl pyrazolines as human acyl-CoA:cholesterol acyltransferase inhibitors
A series of pyrazoline derivatives were prepared for evaluating their acyl-CoA:cholesterol acyltransferase activities. 3-(3,5-Di-tert-butyl-4- hydroxyphenyl)-5-(multi-substituted 4-hydroxyphenyl)-2-pyrazolines 4a-i were shown in vitro inhibitory activity on hACAT-1 and -2.
Jeong, Tae-Sook,Kim, Kyung Soon,An, So-Jin,Cho, Kyung-Hyun,Lee, Sangku,Lee, Woo Song
p. 2715 - 2717
(2007/10/03)
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