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利用生物活性亚结构拼接原理,将活性酰腙亚结构与活性噻唑环亚结构进行拼接,设计合成了14个新型N’-芳基亚甲基-N-(4-取代苯甲酰氧基噻唑-2-基)取代苯甲酰腙衍生物.所有目标化合物经1H NMR、IR、质谱及元素分析等手段进行了表征,部分化合物还经过13C NMR进行了确证.抗肿瘤测试结果表明,该系列化合物表现出明显的抗肿瘤活性,其对人口腔上皮癌细胞株(KB)的抑制活性优于对鼻咽癌细胞株(CNE2)的抑制活性;采用离体平皿法对目标化合物进行杀菌活性测试,测试菌种为:小麦赤霉菌、水稻纹枯霉菌、黄瓜灰霉菌、番茄早疫菌、烟草赤星菌和黄瓜炭疽菌.结果表明,在1.0×10-4 g/m L浓度下,目标化合物对部分菌种表现中等抑菌活性.
In this work, 14 novel N’-arylmethylene-N- (4-substituted benzoyloxythiazoles) have been designed and synthesized by the substructure of active acyl hydrazones and the active thiazole substructures. 2-yl) substituted benzoyl hydrazone derivatives.All the target compounds were characterized by 1H NMR, IR, MS and elemental analysis and some compounds were also confirmed by 13C NMR.Anti-tumor test results showed that the series The compounds showed obvious anti-tumor activity, and their inhibitory activity on human oral epithelial cancer cell line (KB) was better than that on nasopharyngeal carcinoma cell line (CNE2). The bactericidal activity test of the target compound , The tested strains were Gibberella zeae, Fusarium solani, Botrytis cinerea, A. solanacearum, R. solani and Cucumber anthracnose.The results showed that under the concentration of 1.0 × 10-4 g / mL, the target compound Some bacteria showed moderate antibacterial activity.