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Digitale Medien

Leukotriene biosynthesis inhibition by aryl and aroyl substituted naphthoquinones (1991)

Roland, D. M. ; Macchia, W. M. ; Grim, K. S. ; [weitere]

Springer

Inflammation research 34 (1991), S. 145-147

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Details

ISSN: 1420-908X

Quelle: Springer Online Journal Archives 1860-2000

Thema: Medizin

Notizen: Abstract Naphthoquinones are known to inhibit 5-lipoxygenase. In particular, CGS 8515 (methyl 2-[(3,4-dihydro-3,4-dioxo-1-naphthalenyl)amino]benzoate) has been studied in detail. However this potent and selective 5-lipoxygenase inhibitor has a short duration of action and poor bioavailability. To improve the duration of action we have prepared a series of carbon substituted naphthoquinones. Several members of this series have demonstrated potentin vitro inhibition of 5-LO (IC50's〈10−6 M) and at doses of 1 mg/kg iv completely inhibited LTB4 production measured inex vivo A23187-stimulated blood from dogs. The duration of action measured by theex vivo assay was improved up to threefold over CGS 8515.

Materialart: Digitale Medien

URL: http://dx.doi.org/10.1007/BF01993262

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