Synthesis And Study On Bioactivity Of 2-Hydrazono-1.3-Dithiolane

The heterocyclic compounds, whose structures are simple, exist in a large number of pesticides. They play a very important role in researching and exploitation of pesticide. Some research works have discovered "2-hydrazono-1.3-dithiolane" derivatives have good bioactivity. In this paper, the efforts were focused on the design, synthesis and bioactivity test of "2-hydrazono-1.3-dithiolane"' derivatives. A series of useful and creative results have been obtained.The research of Quantitative Structure-Activity Relationships (QSAR), which can predict compound's bioactivity. help to know the pharmaceutical effect and design target molecule (TM). On the basis of free-Wilson model, Three kinds of target molecular owning potential bioactivity are designed.The synthesis of "2-hydrazono-1.3-dithiolane". the key intermediate has been improved first. Compared with previous synthetic methods. The new method using Ultrasound irradiation is more convenient and easily-controlled. The reaction time is shorten 4-5 times than that of classical method. And the yield is higher.Forty-one compounds have been synthesized; among them twenty-two are intermediates, and nineteen are target compounds. There are thirteen new compounds of the targets molecular. These new compounds"chemical structures were confirmed by IR. 1HNMR MS and/or element analysis.The preliminary bioactivity test of the target compounds have been carried out. The results showed that five compounds (2c, 2d, 6f, 7g and 7h) of the "2-hydrazono-1.3-dithiolane" derivatives had good biological activity on escherichia (10407) and streptococcus (1123). Especially, the MIC of 2c and 2d are 16mg L. equal to SMZ and CET. Their LD50 are 2258.37 438.61mg/kg (calculated on Bliss.2c) and 2782.9 605.94mg kg (calculated on Bliss.2d). Therefore, the toxicity is lower.What's more, 6f, 7g and 7h have good bioactivity on pyricularia oryza, fusarium moniliforme, and xanthomonas oryza and sclerotinia sclerotiorum. Especially. 6f have a very good protecting effect on xanthomonas oryza and the average is 76.04%. it is higher than the normal pesticide's (43.07%).These results had offered a good basis for the practical application research.