4-Hydroxythiazole inhibitors of 5-lipoxygenase

FAJ Kerdesky, JH Holms, JL Moore…

Index: Kerdesky, Francis A. J.; Holms, James H.; Moore, Jimmie L.; Bell, Randy L.; Dyer, Richard D.; et al. Journal of Medicinal Chemistry, 1991 , vol. 34, # 7 p. 2158 - 2165

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Citation Number: 32

Abstract

4-Hydroxythiazoles have been identified as potent inhibitors of 5-lipoxygenase in vitro exhibiting ICm's of less than 1 fiM. 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 ...