Abstract
The authors have synthesised a series of thiourea and benzamide compounds and claim their use as potential anti-inflammatory and/or anti-atherosclerotic drugs. 280 Compounds were synthesised and tested for lipoxygenase (LO) inhibitory activity in an in vitro assay system using the purified rabbit reticulocyte 15-LO. Some of them were shown to be potent LO inhibitors with IC50 values as low as 2 nM. In an in vitro model of inflammation, several compounds inhibited monocyte recruitment with an EC50 in the lower μM-range and some inhibitors slowed down the development of atherosclerotic lesions in an animal atherosclerosis model. However, there was no correlation between LO inhibition and anti-atherogenic or anti-inflammatory activity.