2-羟基-3-硝基-1,4-萘醌的合成及其抗过敏活性

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

作者信息

Buckle D R, Cantello B C, Smith H, Smith R J, Spicer B A

出版信息

J Med Chem. 1977 Aug;20(8):1059-64. doi: 10.1021/jm00218a014.

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 most potent compounds were 7c and 7e which produced a 50% inhibition in the rat PCA test at doses of about 10 micrometerM/kg following subcutaneous 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 micrometerM/kg.

摘要

一系列新型2-羟基-3-硝基-1,4-萘醌被证明是大鼠被动皮肤过敏反应（PCA）的有效抑制剂，并且在C-6和C-7处进行烷基取代时具有最高的效力。最有效的化合物是7c和7e，皮下给药后，在大鼠PCA试验中，约10微摩尔/千克的剂量可产生50%的抑制作用，口服给药后也显示出活性。相关的4-羟基-3-硝基-2(1H)-萘醌在高达500微摩尔/千克的剂量下对大鼠PCA没有影响。