摘要
[目的]合成查尔酮类似化合物,并研究其抑菌活性,以寻找高效、安全的抑菌活性化合物。[方法]以苯甲酰氯类化合物和胺类化合物为原料,通过酰氯的胺解反应设计并合成了16种查尔酮类似化合物,对其分子结构经红外光谱(IR)和氢核磁共振波谱(1H NMR)进行确认。[结果]该类化合物具有一定的抑菌活性,当浓度为100 mg/L时,化合物A2(2-氯-N-苯基苯甲酰胺)对水稻纹枯病(Rhizoctonia solani)和油菜菌核病菌(Sclerotiua sclerotiorum)的抑制率分别达90.27%和92.56%。[结论]产物A2为查尔酮的类似化合物,且属于天然产物,在自然界中能够自然降解,不会引起环境污染;而且其化学结构简单,人工合成也比较容易,可以以此为先导化合物对其结构进行优化和改造;研究其结构和活性之间的关系,开发出高效、低毒、对非靶标生物安全的新型抑菌剂。
[Objective] To synthesize chalcone analogues and study their antifungal activity so as to find high-efficient and safe compounds with antifungal activity.[Method] With benzoyl chloride compounds and amines as the materials,16 chalcone analogues were designed and synthesized through the aminolysis reaction of acyl chloride,and their molecular structures were determined by IR and 1H NMR.[Result] The chalcone analogues had certain antifungal activity.The antifungal rate of 100 mg/L compound A2（2-chloro-N-phenyl benzamide） against Rhizoctonia solani and Sclerotiua sclerotiorum reached 90.27% and 92.56%,respectively.[Conclusion] Product A2 was an analogue of the natural product chalcone that could naturally degrade without causing environmental pollution.What＇s more,its chemical structure was simple and easy to prepare.Using A2 as a lead compound,new high-efficient and low-toxic antifungal agents which were safe to the non-target organisms could be developed through optimizing its chemical structure and studying the relationship between structure and activity.
出处
《安徽农业科学》
CAS
北大核心
2011年第27期16551-16553,16556,共4页
Journal of Anhui Agricultural Sciences
基金
西华大学有机化学重点学科项目
关键词
查尔酮类似化合物
合成
水稻纹枯病
油菜菌核病菌
抑菌活性
Chalcone analogues
Synthesis
Rhizoctonia solani
Sclerotinia sclerotiorum
Antifungal activity
