Derivative Synthesis And Antifungal Activity Evaluation Of Antimicrobial Active Components Of Bamboo Extract

This paper mainly bamboo extract and flavonoids bactericidal active ingredient cinnamic compounds as the main molecular skeleton,based on the pharmacophores that were found in the previous work and reported in the literature to have a good inhibitory effect,19 novel flavone Mannich bases and 14 novel pyrazole cinnamate amide derivatives were designed.All the compounds were selected through the synthesis route and optimized in the process,which made the raw materials easily accessible,the reaction operation was simple,and the yield was high.The structure and configuration were determined by 1H NMR,13CNMR and MS.(1)Evaluation of antifungal activities of 19 flavonoids Mannich base derivatives.The results of antifungal activity evaluation indicates compound 3,5,7-Trihydroxy-2-(4-hydroxyphenyl)-8-(((4-methoxybenzyl)amino)methyl)-4H-chromen-4-one(5q)exhibited the best antifungal activity with EC50 values of 67.5 mg/L against Gaeumannomycesgramini and compound 3,5,7-trihydroxy-2-(4-hydroxyphenyl)-8-(((4-methylbenzyl)amino)methyl)-4H-chromen-4-one(5p)exhibited the best antifungal activity with EC50 values of 147.7 mg/L against Gibberella sanbinetti.In addition,we provide a valuable reference for the introduction of carbohydrate in flavone.(2)The antifungal activity of 14 substituted pyrazole cinnamate derivatives was evaluated.The results show that the antifungal activity of different target compounds of the substituents on the structure of cinnamic acid will change.When the target compound Ri is 2-substituted OCH3 and R2 is H,the antifungal activity of the target compound(E)-N-(4-Cyano-l-phenyl-1H-pyrazol-5-yl)-3-(2-methoxyphenyl)acrylamide(3b)is the best,and the inhibition rate against Tomato Rhizoctonia solaniand and Pear anthracnose is 26.13%and 30.81%at 50 mg/L.In this paper,19 Mannanich base derivatives containing benzylamine moiety were synthesized by Mannich reaction using flavonoids as templates.Two compounds were screened out to have good activity against Gaeumannomyces gramini and Gibberella sanbinetti.An innovative synthesis of 14 cinnamamide compounds containing a pyrazole moiety was used to screen for a compound with a relatively active activity against Tomato Rhizoctonia solaniand and Pear anthracnose.The results provide valuable references for the development of novel antifungal drugs for flavonoid derivatives and cinnamic acid derivatives.