期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 22, 期 8, 页码 2396-2402出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2014.03.008
关键词
3,5-Dinitrobenzoate; 5-Lipoxygenase inhibitors; Cell-free assay; Human whole blood assay; SAR study
资金
- Ministry of Science and Technology of China [2012AA020308, 2009CB918503]
- Natural Science Foundation of China [20873003, 11021463]
Human 5-lipoxygenase (5-LOX) is a well-validated target for anti-inflammatory therapy. Development of novel 5-LOX inhibitors with higher activities is highly demanded. In previous study, we have built a model for the active conformation of human 5-LOX, and identified naphthalen-1-yl 3,5-dinitrobenzoate (JMC-4) as a 5-LOX inhibitor by virtual screening. In the present work, 3,5-dinitrobenzoate-based 5-lipoxygenase inhibitors were developed. Twenty aryl 3,5-dinitrobenzoates, N-aryl 3,5-dinitrobenzamides and analogues were designed and synthesized. Several of them were found with significantly increased activities according to cell-free assay and human whole blood assay. The structure-activity relationship study may provide useful insights for designing effective 5-LOX inhibitors. (C) 2014 Elsevier Ltd. All rights reserved.
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