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Indazolinones, a new series of redox-active 5-lipoxygenase inhibitors with built-in selectivity and oral activity

P Bruneau, C Delvare, MP Edwards…

文献索引:Bruneau; Delvare; Edwards; McMillan Journal of Medicinal Chemistry, 1991 , vol. 34, # 3 p. 1028 - 1036

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被引用次数: 68

摘要

Methemoglobin (MHb) induction by 21a in dog blood precluded its development for clinical use. Attempts at dissociating 5-LPO inhibitory properties and MHb formation showed that MHb formation in vitro seemed to be related to the redox potential of the compounds whereas 5-LPO inhibition was not. This study led to a series of 4-(Nn-pentylcarbamoyl) indazolinones which maintained in vitro 5-LPO potency but did not induce MHb.