Synthesis and 5-lipoxygenase inhibitory activity of 5-hydroperoxy-6, 8, 11, 14-eicosatetraenoic acid analogs
FAJ Kerdesky, SP Schmidt, JH Holms…
Index: Kerdesky; Schmidt; Holms; Dyer; Carter; Brooks Journal of Medicinal Chemistry, 1987 , vol. 30, # 7 p. 1177 - 1186
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Citation Number: 49
Abstract
A series of eicosatetraenes (2-24) were designed, synthesized, and evaluated in vitro for inhibitory activity against 5-lipoxygenase (20000g supernatant from homogenized rat basophilic leukemia cells). All compounds were found to be active with the potencies (IC5; s) ranging from 0.19 to 97 wM. Compounds containing the hydroxamic acid functionality (10- 12) exhibited the best activity (IC6o= 0.19-2.8 wM). The most potent inhibitor was 5-[[(hy- ...
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