中文摘要：

目的设计合成新型酰腙席夫碱类化合物,并评价其体外抗结核分枝杆菌活性。方法以羟基苯甲醛为起始原料,经酰肼化、脱水缩合反应制备目标化合物,其结构均经MS和-1H-NMR分析确证。采用平皿二倍稀释法测定目标化合物体外抗结核杆菌标准株（H37Rv）的最小抑菌浓度（MIC）。结果合成20个新型酰腙席夫碱类化合物,部分化合物具有一定的抗结核活性,其中化合物b1-b5具有较好的体外抗结核分枝杆菌活性,化合物b2、b3和b5体外抗结核分枝杆菌活性（MIC〈0.125μg/ml）是先导化合物IMB-HC109（MIC=0.25μg/ml）的2倍以上。结论目标化合物结构中A部分含有2-吡啶羰基或4-吡啶羰基片段,B部分含有3-苯甲醚或4-苯甲醚片段,C部分含有吡啶基片段有利于提高该类化合物体外抗结核活性,其中化合物b2、b3和b5的体内抗结核分枝杆菌活性值得进一步研究。

英文摘要：

Objective To design, synthesize and evaluate the in vitro antituberculosis activity of novel acylhydrazone schiff base derivatives. Methods The title compounds were synthesized from hydroxy benzaldehyde, via hydrazide reaction and condensation reaction. The structure were confirmed by MS and -1H-NMR. The MICs of antituberculosis activity（H37Rv） were determined by standard agar dilution method. Results Twenty novel compounds were synthesized, among which compounds b1-b5 were found to have potential antituberculosis activity. Specifically, the activities of compounds b2, b3 and b5（MIC 〈0.125 μg/ml） were two folds stronger than that of the lead compound IMB-HC109（MIC = 0.25 μg/ml）. Conclusion In the title compounds structure, part A bearing 2-pyridyl or 4-pyridyl carbonyl fragments, part B with 3-or 4-methyl-phenoxide fragments, and part C containing pyridyl group can improve in vitro antituberculosis activity. The in vivo antituberculosis activities of compounds b2, b3 and b5 merit further investigation.