Abstract: In search of pesticide lead compound with new structure type, eleven novel 2-methylthio-1-phenylethanone benzoylhydrazones were designed and synthesized by reacting 2-methylthio substituted acetophenone with substituted benzoylhydrazones. Their structures were confirmed by MS, 1H NMR and elemental analysis. The preliminary bioassay showed that some of title compounds had fungicidal activities or insecticidal activities, for example, 2-methylthio-1-(4-methylphenyl)ethanone 4-chloro-benzoylhydrazone exhibited more than 95% inhibition against Botrytis cinerea and Gibberella zeae at 500 mg/L.