131786-51-1Relevant articles and documents
4-HYDROXYTHIAZOLES AS 5-LIPOXYGENASE INHIBITORS
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, (2008/06/13)
A composition for the inhibition of lipoxygenase enzymes comprising a pharmaceutically acceptable carrier and a compound of the formula: I wherein R1 and R2 are independently selected from the group consisting of alkyl, alkenyl, cycloalkyl, cycloalkenyl,
4-Hydroxythiazole Inhibitors of 5-Lipoxygenase
Kerdesky, Francis A. J.,Holms, James H.,Moore, Jimmie L.,Bell, Randy L.,Dyer, Richard D.,et al.
, p. 2158 - 2165 (2007/10/02)
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.
