Processes · 2020 · 10 citations · 18 references
Life SciencesBiologyMicrobiologyDrug DiscoveryMycologyPlant BiochemistryAntifungal AgentsEnzyme InhibitionFungal BiochemistryFungal MetabolismFungal PathogenesisFungal Secondary MetabolitesBotanical FungicidesFungal Cell Wall BiologyFungal Cell Wall Targeting DrugsFungal Enzyme InhibitorsFungicide ChemistryMaleimide ChemistryNew Antifungal AgentsPlant-derived Fungicides
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.
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Atul R. Gholap, Kiran S. Toti, Fazal Shirazi et al. · Bioorganic & Medicinal Chemistry · 2007 · 136 citations
Studies on Polyoxins, Antifungal Antibiotics
Kiyoshi Isono, Junsaku Nagatsu, Kimie Kobinata et al. · Agricultural and Biological Chemistry · 1967 · 88 citations · Full text