Abstract
Chitin is an important part of the fungal cell wall, but is not found in plants and mammals, so chitin synthase (CHS) can be a green fungicide target. In this paper, 35 maleimide compounds were designed and synthesized as CHS inhibitors. All the screened compounds showed different degrees of CHS inhibitory activity and antifungal activity in vitro. In particular, the half–inhibitory concentration (IC50) value of compound 20 on CHS was 0.12 mM, and the inhibitory effect was better than that of the control polyoxin B (IC50 = 0.19 mM). At the same time, this compound also showed good antifungal activity and has further development value.
Highlights
Fungal infections are a worldwide threat to agricultural economy and human health [1,2]
A polymer of N-acetylglucosamine conjugated by β-1,4 glycoside bonds, is an essential structural polysaccharide found in all fungal cell walls but not in vertebrates and plants [4]
We summarized designed, synthesized series of1 maleimide compounds
Summary
Fungal infections are a worldwide threat to agricultural economy and human health [1,2]. Effective and safe antifungal drugs are very limited, and drug resistance risks are on the rise. A polymer of N-acetylglucosamine conjugated by β-1,4 glycoside bonds, is an essential structural polysaccharide found in all fungal cell walls but not in vertebrates and plants [4]. The earliest research on CHS inhibitors dates back to the late 1950s. Isono et al isolated and extracted polyoxin from streptomycin, and found that it can inhibit the growth and reproduction of fungi by reducing the synthesis of chitin [6]. Researchers have successively screened and obtained a variety of compounds that have a mild inhibitory effect on CHS by separation from natural products, extraction from plants, or chemical synthesis
Sign-in/Register to view highlights & summary 
Published Version (
Free)
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call