ANTITUBERCULOSIS ACTIVITY OF SOME NITROFURAN DERIVATIVES
ANTITUBERCULOSIS ACTIVITY OF SOME NITROFURAN DERIVATIVES
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DOI：
10.1111/j.2042-7158.1969.tb08283.x
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发表时间：
1969-01-01
影响因子：
3.3
通讯作者：
VISCHER, W
中科院分区：
文献类型：
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作者：
BRUHIN, H;BUHLMANN, X;VISCHER, W
合成了一系列4，6-二取代2-（5-硝基亚糠基肼基）-1，3，5-三嗪类化合物。部分化合物对结核分枝杆菌具有较好的体外抗菌活性，体内抗菌活性中等（与临床使用的化合物相比，体内抗菌活性仅在高剂量下观察到，且结果也不规则）。最具活性的化合物是5-硝基-2-糠醛的三嗪基腙，其中三嗪环被两个氨基取代，其中至少一个是（α-支链烷基）-或环烷基胺。讨论了这些化合物的结构-抗结核活性关系。
A series of 4,6‐disubstituted 2‐(5‐nitrofurfurylidenehydrazino)‐1,3,5‐triazines has been synthesized. Some of these compounds possessed good antibacterial activity againstMycobacterium tuberculosis in vitroand moderate activityin vivo(the activityin vivowas observed only with high dosages compared with compounds in clinical use and the results were also irregular). The most active compounds are triazinylhydrazones of 5‐nitro‐2‐furaldehyde in which the triazine ring is substituted with two amino‐groups, at least one of which is an (α‐branched chain alkyl)‐ or cycloalkylamine. Structure‐ anti‐tuberculosis activity relations for these compounds are discussed.