Synthesis And Biological Activity Of Pentadienone And Chalcone Derivatives Containing Sulfonylpiperazin

Bioactive molecules from biological resources,especially natural products of plant origin,offer unlimited opportunities for the development of new drugs,food additives or cosmetic ingredients.Using natural products as lead compounds is an effective method for pesticide discovery.Piperazine skeleton is a potential active intermediate,and has a strong development potential and application prospect.In view of this,sulfonyl piperazine structure was introduced into the structure of pentadienone and chalcone,and a series of sulfonyl piperazine-containing pentadienone and chalcone compounds were designed and synthesized.The main research work of this paper is summarized as follows:1.20 novel chalcone derivatives containing piperazine fragment were designed and synthesized.Their fungicidal activities and preliminarily action mechanism against R.solani were evaluated.Strikingly,the biological activity compound D2 was obtained by optimizing the structure of the system.Subsequently,the practical value of D2 was ascertained by the relative surveys on the in vivo anti-R.solani.The results were revealed by scanning electron microscope demonstrated that D2 could induce the irregular and shrivelled growth of mycelium,and rupture of mycelium surface.This study indicates that chalcone derivatives containing piperazine skeleton had better inhibitory effect on plant fungi,providing further complementary research on new pesticides.2.24 novel 1,4-pentadien-3-one derivatives containing sulfonamide moiety were conceived,and their antifungal,antibacterial and antiviral activities were evaluated.The bioassay result showed that most compounds exhibited excellent fungicidal activity in vitro at 100μg/m L.Compounds E6,E8 and E13 were found and presented more potent fungicidal activity than azoxystrobin.The target compounds showed striking inhibitory effects against Xoo,Rs,Xcm,Pcb and Ac.The EC₅₀value exhibited that E5(EC₅₀=10.99μg/m L)had better antibacterial activity against Xoo than BT(EC₅₀=118.5μg/m L)and TC(EC₅₀=105.3μg/m L).The results of anti-TMV demonstrated that E17 had a good in vivo antiviral effect compared with ningnanmycin.The activity of E17 was further verified by MST.3.Together,the study indicates that chalcone derivatives containing piperazine skeleton had better inhibitory effect on plant fungi,providing further complementary research on new pesticides.The results gained from this study suggest that 1,4-pentadien-3-one derivatives containing sulfonyl piperazine skeleton had great potential application in antifungal,antibacterial and antiviral agent industry.The results of these studies suggest that the use of active splicing can improve the biological activity of natural compounds and provide an indispensable further complement to the development of novel pesticides.