2-Substituted-1-naphthols as potent 5-lipoxygenase inhibitors with topical antiinflammatory activity

…, GD Maynard, JJ Petraitis, JE Shaw…

Index: Batt; Maynard; Petraitis; Shaw; Galbraith; Harris Journal of Medicinal Chemistry, 1990 , vol. 33, # 1 p. 360 - 370

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Citation Number: 64

Abstract

The synthesis, biological evaluation, and structure-activity relationships of a series of 1- naphthols bearing carbon substituents at the 2-position are described. These compounds are potent inhibitors of the 5-lipoxygenase from RBL-1 cells and also inhibit bovine seminal vesicle cyclooxygenase. Structureactivity relationships for these two enzymes are different, implying specific enzyme inhibition rather than a nonspecific antioxidant effect. 2-( ...