Journal of Medicinal Chemistry p. 2158 - 2165 (1991)
Update date:2022-08-04
Topics:
Kerdesky, Francis A. J.
Holms, James H.
Moore, Jimmie L.
Bell, Randy L.
Dyer, Richard D.
et al.
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.
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