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

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Title
Novel 3,5-diaryl pyrazolines and pyrazole as low-density lipoprotein (LDL) oxidation inhibitor
Author(s)
Tae Sook Jeong; Kyung Soon Kim; Ju Ryoung Kim; Kyung Hyun Cho; Sangku LeeWoo Song Lee
Bibliographic Citation
Bioorganic & Medicinal Chemistry Letters, vol. 14, no. 11, pp. 2719-2723
Publication Year
2004
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.
Keyword
LDL-antioxidant
ISSN
0960-894X
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/j.bmcl.2004.03.072
Type
Article
Appears in Collections:
Division of Biomaterials Research > Industrial Bio-materials Research Center > 1. Journal Articles
Ochang Branch Institute > Anticancer Agent Research Center > 1. Journal Articles
Jeonbuk Branch Institute > Functional Biomaterial Research Center > 1. Journal Articles
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