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Abstract
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.