99107-53-6Relevant academic research and scientific papers
1,4-Dihydronaphthoquinones, hydroindoloquinones, benzofurans, and benzothiophenes as inhibitors of 5-lipoxygenase. Synthesis and structure-activity studies
Yamashita,Schaub,Back,White,Toy,Ghazal,Burdick,Brashler,Holm
, p. 775 - 781 (1990)
A series of substituted 1,4-dihydronaphthoquinones, hydroindoloquinones, benzofuran-4,7-dihydroquinones, and benzothiophene-4,7-dihydroquinones were synthesized and evaluated for inhibitory activity against 5-lipoxygenase. These compounds were found to be active in vitro for LTC4/D4 inhibition with the potencies (IC50's) ranging from 0.2 to 85 μM. Active 1,4-dihydronaphthoquinone acetates (IC50 4 inhibition assay. The acetates of 1,4-dihydronaphthoquinones containing the alkyl substituent(s) (2-n-butyl, 11, and 2,3-diethyl, 15) exhibited the best activity in LTC4/D4 inhibition (IC50 = 0.2-0.4 μM, in vitro) as well as in LTB4 inhibition (60-75% inhibition).
Substituted naphthalenes, indoles, benzofurans and benzothiophenes as lipoxygenase inhibitors
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, (2008/06/13)
The present invention relates to substituted naphthalenes, indoles, benzofurans and benzothiophenes (many of which are novel) which are useful as inhibitors of the synthesis of leukotrienes and as inhibitors of the action of lipoxygenase in mammalian metabolism
Substituted naphthalenes, indoles, benzofurans, and benzothiophenes as lipoxygenase inhibitors
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, (2008/06/13)
The present invention provides certain novel substituted naphthalenes, indoles, benzofurans, and benzothiophenes of Formula I which are useful as inhibitors of leukotriene biosynthesis and as inhibitors of lipoxygenase. They are thus employed wherever it is medically necessary or desirable to inhibit these systems. STR1
