ISSN:
1420-908X
Source:
Springer Online Journal Archives 1860-2000
Topics:
Medicine
Notes:
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.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF01993262
