Synthesis And Bioactivities Evaluation Of Novel DHODH Inhibitor4-thiazolone Analogues

Base on the structure of4-thiazolone, two series of47compounds were designed and synthesized, and the chemical structures were characterized by1H,13C NMR, HRESI and IR. The bioactivities of some of these compounds were tested as DHODH inhibitor by CoQO method. It was observed that the halogen substituted derivatives had better inhibition activities against DHODH than other electron-withdrawing or electron-donating substituents, in addition, the test results also suggested that biphenyl substituents compounds showed higher DHODH inhibition activities than phenyl substitutes. IC50value of IPP173103, IPP173104, IPP173108, IPP173109and IPP173116reached to nm level. Furthermore, heterocycle, naphthalene, diphenyl ether and diphenyl amide substituents, and the diphenyl amide analogues were tested to investigate the relationship between the structure and bioactivities. In addition, the two-way research and development of pharmceuticals and pesticides is the important step of the finding of leading compounds. Some of the compounds were tested the bioactivities against plant root-knot nematode, and the growth of nematode was inhibited obviously by these two series of compounds. The inhibition rate of IPP173204, IPP173015, IPP173101and IPP173001was above90%when the concentration was30-40ppm, and no obvious toxic effect were observed on plants.