Abstract
The high incidence of fungal pathogens has become a global issue for crop protection. A promising strategy to control fungal plant infections is based on the use of nature-inspired compounds. The cytochrome bc1 complex is an essential component of the cellular respiratory chain and is one of the most important fungicidal targets. Natural products have played a crucial role in the discovery of cytochrome bc1 inhibitors, as proven by the development of strobilurins, one of the most important classes of crop-protection agents, over the past two decades. In this review, we summarize advances in the exploration of natural product scaffolds for the design and development of new bc1 complex inhibitors. Particular emphasis is given to molecular modeling-based approaches and structure–activity relationship (SAR) studies performed to improve the stability and increase the potency of natural precursors. The collected results highlight the versatility of natural compounds and provide an insight into the potential development of nature-inspired derivatives as antifungal agents.
Highlights
Plant diseases caused by fungal pathogens are a major threat to the agricultural industry worldwide
Natural products have played a crucial role in the investigation of cytochrome bc1 inhibitors, In this review, we summarize the efforts towards the exploration of natural product scaffolds leading to the discovery of one of the most important classes of crop-protection agents, the strobilurins
The major drawbacks of these fungicides are their toxicity to aquatic organisms and the increased number of fungal pathogens that are showing occurrence of resistance, mainly due to Strobilurins are natural compounds isolated for the first time in 1977 from basidiomycetes
Summary
Plant diseases caused by fungal pathogens are a major threat to the agricultural industry worldwide. Via the Rieske iron–sulfur protein and cytochrome c1, to cytochrome c, while the second electron passes through two b-type haems (bL and bH ) to reduce ubiquinone at the Qi site [2] This process results in proton translocation and generates the proton motive force required in the production of ATP. Natural products, with their enormous structural diversity, are an invaluable source of inspiration in the design and development of new biologically active compounds [3]. Molecular modeling-based approaches and structure–activity relationship (SAR) studies performed several millennia to acquire specific ligand–protein binding motifs, these privileged compounds serve to improve the potency, selectivity, and stability of bioactive natural products are highlighted as as important, biologically pre-validated platforms for the development of new leads in medicinal well. Toxicity against germinating fungal spores and relatively low toxicity for terrestrial animals
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