Abstract
Thirty-six novel threoninamide carbamate derivatives were designed and synthesised using active fragment-based pharmacophore model. Antifungal activities of these compounds were tested against Oomycete fungi Phytophthora capsici in vitro and in vivo. Interestingly, compound I-1, I-2, I-3, I-6 and I-7 exhibited moderate control effect (>50%) against Pseudoperonospora cubensis in greenhouse at 6.25 μg/mL, which is better than that of control. Meanwhile most of these compounds exhibited significant inhibitory against P. capsici. The other nine fungi were also tested. More importantly, some compounds exhibited remarkably high activities against Sclerotinia sclerotiorum, P. piricola and R. solan in vitro with EC50 values of 3.74–9.76 μg/mL. It is possible that the model is reliabile and this method can be used to discover lead compounds for the development of fungicides.
Highlights
Oomycete fungi can cause several destructive diseases in crops, vegetables and fruits, such as Phytophthora infestans, Peronospora hyoscyami, Phytophthora capsici and Pseudoperonospora cubensis[1]
In this paper, based on the structure of seven commercialised carboxylic acid amide (CAA) fungicides, we found that they have similar structural fragments: amide bond, para-substituted phenyl, 3,4-dialkyloxy substituted phenyl
The key technical challenge for this approach was the detection of fragment hits
Summary
Oomycete fungi can cause several destructive diseases in crops, vegetables and fruits, such as Phytophthora infestans, Peronospora hyoscyami, Phytophthora capsici and Pseudoperonospora cubensis[1]. The compound was found to display higher in vitro antifungal activities against P. capsici
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