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Background  Plant fungi (e.g.,  Pellicularia sasakii, Gibberella zeae, Fusarium oxysporum,  and  Cytospora mandshurica  and  Phytophthora infestans ) and bacteria (e.g.,  Ralstonia solanacearum ) are extremely difficult to manage in agricultural production. The high incidence of plant mortality and the lack of effective control methods make  P. sasakii  and  R. solanacearum  two of the world’s most destructive plant pathogens. Pathogenic fungi and bacteria are responsible for billions of dollars in economic losses worldwide each year. Thus, we designed an active amide structure and synthesized a series of novel amide derivatives containing a triazole moiety to discover new bioactive molecules and pesticides that can act against fungi and bacteria.    Results  A series of amide derivatives containing a triazole moiety were synthesized. All the obtained compounds were characterized through proton and carbon nuclear magnetic resonance spectroscopy, infrared spectroscopy, and elemental analysis. Preliminary antifungal activity test showed that some of the synthesized compounds exhibited moderate antifungal activity against  P. sasakii ,  G. azeae ,  F. oxysporum ,  C. mandshurica , and  P. infestans  at 50 mg/L. Compound  4u  displayed more potent antifungal activity against  P.  sasakii and  G. azeae  than hymexazol. Preliminary antibacterial activity results showed that some of the synthesized compounds exhibited high anti-bacterial activity against  R. solanacearum  at 200 mg/L. Compounds  4m  and  4q  displayed high antibacterial activity against  R. solanacearum , with 71% and 65% inhibitory rates, respectively.    Conclusions  A series of novel amide derivatives containing 1,2,4-triazole moiety were synthesized through the reaction of intermediate  3  with different acyl chlorides and anhydrous potassium carbonates in anhydrous tetrahydrofuran at 50°C, using 2,4-dichloroacetophenoneas as a starting material. The title compounds exhibited high inhibitory effects against  P. sasakii ,  R. solanacearum , and  G. azeae .

Synthesis, antifungal and antibacterial activity for novel amide derivatives containing a triazole moiety