4-Hydroxythiazole Inhibitors of 5-Lipoxygenase

Article abstract of DOI:10.1021/jm00111a035

4-Hydroxythiazoles have been identified as potent inhibitors of 5-lipoxygenase in vitro exhibiting IC50's of less than 1 μM.An investigation of structure-activity relationships showed that the most potent inhibitors of this series are the 5-phenyl derivatives.The corresponding thiazolidin-4-one analogues were found to be relatively inactive.The 4-hydroxythiazoles were active inhibitors against 5-lipoxygenase in both intact rat polymorphonuclear leukocytes and human whole blood.The compounds were also selective inhibitors of 5-lipoxygenase, displaying only weak activity against other related enzymes, cyclooxygenase and 12- and 15-lipoxygenase.