ChemInform Abstract: 1,4-Dihydronaphthoquinones, Hydroindoloquinones, Benzofurans, and Benzothiophenes as Inhibitors of 5-Lipoxygenase. Synthesis and Structure-Activity Studies

Autor:	Michael D. Burdick, Ayako Yamashita, Gordon J. White, M. S. Holm, Robert G. Schaub, N. B. Ghazal, A. Toy, John R. Brashler, Michael K. Bach
Rok vydání:	1990
Předmět:	chemistry.chemical_classification biology Stereochemistry Substituent General Medicine Inhibitory postsynaptic potential In vitro chemistry.chemical_compound chemistry Arachidonate 5-lipoxygenase biology.protein lipids (amino acids peptides and proteins) IC50 Alkyl Ex vivo
Zdroj:	ChemInform. 21
ISSN:	0931-7597
DOI:	10.1002/chin.199025147
Popis:	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 microM. Active 1,4-dihydronaphthoquinone acetates (IC50 less than 20 microM) were evaluated in an ex vivo LTB4 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 microM, in vitro) as well as in LTB4 inhibition (60-75% inhibition).
Databáze:	OpenAIRE
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