Synthesis and antifungal activity evaluation of new heterocycle containing amide derivatives

Abstract

A series of heterocycle containing amide derivatives (1–28) were synthesised by the combination of acyl chlorides (1a, 2a) and heterocyclic/homocyclic ring containing amines, and their in vitro antifungal activity was evaluated against five plant pathogenic fungi, namely Gibberella zeae, Helminthosporium maydis, Rhizoctonia solani, Botrytis cinerea and Sclerotinia sclerotiorum. Results of antifungal activity analysis indicated that some of the products showed good to excellent antifungal activity, as compound 2 showed excellent activity against G. zeae and R. solani and potent activity against H. maydi, B. cinerea and S. sclerotiorum, and compounds 1, 8 and 10 also displayed excellent antifungal potential against H. maydi, B. cinerea and S. sclerotiorum and good activity against R. solani when compared with the standard carbendazim.

Graphical Abstract

Keywords:

• synthesis
• amide derivatives
• plant pathogenic fungi
• antifungal activity

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This project was supported by the Scientific Research Fund of Sichuan Provincial Education Department [grant number 13ZA0206]; the Key Scientific Research Fund of Xihua University [grant number Z1013314]; the Innovation Fund of Postgraduate of Xihua University [grant number YCJJ 2014130]; the Research Center for Advanced Computation, Xihua University.