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暗罗素不仅是新结构类型的抗疟活性成分,而且具有广谱抗菌作用。为寻找副作用小、疗效高的抗菌新药,作者对暗罗素的结构进行了改造,并合成了一系列类似物。经体外抗菌试验,其中以吡硫霉净的效果最好。本品对费氏志贺氏菌等11种常见细菌的MIC范围为0.63～8μg/ml;对红色癣菌和白念菌等17种常见真菌的MIC范围为0.25～80μg/ml;与益康唑同时对照试验,10种常见真菌中有9种真菌的MIC低于益康唑。本品是以2-氨基吡啶为开饴原料,经六步反应合成的,总收率为37.6％。本品及前体的熔点、光谱分析等均与文献相符。首次制成剂型治疗表浅真菌病320例,总有效率94％。
Dark Russell is not only a new structural type of anti-malarial active ingredient, but also has a broad-spectrum antibacterial effect. In order to find new antibacterial drugs with low side effect and high curative effect, the author has reformed the structure of dark Russell and synthesized a series of analogues. Antibacterial tests in vitro, of which the best net pyrrolopyrazole effect. This product against Shigella Shigella and other 11 kinds of common bacteria MIC range 0.63 ~ 8μg / ml; against Trichophyton rubrum and white fungi and other 17 kinds of common fungi MIC range of 0.25 ~ 80μg / ml; and econazole In the azole simultaneous control trial, 9 of the 10 common fungi showed lower MICs than econazole. This product is 2-aminopyridine as raw material, synthesized by six steps, the total yield was 37.6%. This product and the precursor melting point, spectral analysis, etc. are consistent with the literature. For the first time made formulations of superficial mycosis in 320 cases, the total efficiency of 94%.