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Title 

Novel 3,5-diaryl pyrazolines and pyrazole as low-density lipoprotein (LDL) oxidation inhibitor

Authors 

Tae Sook JeongKyung Soon KimJu Ryoung KimKyung Hyun ChoSangku LeeWoo Song Lee

Publisher 

Elsevier

Issue Date 

2004

Citation 

Bioorganic & Medicinal Chemistry Letters, vol. 14, no. 11, pp. 2719-2723

Keywords 

LDL-antioxidantapolipoprotein B100oxidized low density lipoproteinIC 50lipid oxidationinhibitory concentration 50lipid peroxidationlipoproteins, LDLoxidation-reductionpyrazoles

Abstract 

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.

ISSN 

0960-894X

Link 

http://dx.doi.org/10.1016/j.bmcl.2004.03.072

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


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