Synthesis and antiallergic activity of 2-hydroxy-3-nitro-1,4-naphthoquinones

Abstract
A selection of novel 2-hydroxy-3-nitro-1,4-naphthoquinones are shown to be potent inhibitors of rat passive cutaneous anaphylaxis (PCA) and to have highest potency with alkyl substitution at both C-6 and C-7. The 2 most potent compounds produced a 50% inhibition in the rat PCA test at doses of about 10 .mu.M/kg following s.c. administration and showed activity after oral administration. Related 4-hydroxy-3-nitro-2(1H)-naphthalenones had no effect on rat PCA in doses up to 500 .mu.M/kg.

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