Synthesis Of Novel N-Aryl Substituted Pyrazole-Containing Derivatives And Their Bioactivities

Pyrazole is an important block to build bioactive compounds in new drug discovery.Compounds with pyrazole moiety always display extensive biological activities.N-Arylpyrazole as a significant part has attracted worldwide attention of organic chemists.Derivatives based on this structure also have diverse biological activities,which might be contribute to the discovery of lead compounds in medicinal and pesticidal fields.Three series of novel N-Arylpyrazole derivatives were designed and synthesized.Their bioactivities were evaluated and some of the compounds exhibited initial biological activities of DHODH inhibition.Compound A20,B15,C10 achieved 1.2 ?M,1.9 ?M,1.25 ?M of IC50 against DHODH respectively.Moreover,some of them also displayed nematode inhibition activities,for example A14,A16 showed 100%inhibition against meloidogyne incognita at 10 ?g/mL.These derivatives might be further optimized as potential lead compounds.