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- W4237217424 abstract "<List> <ListItem><ItemContent> • Developed a two-step synthetic route to anti-plant-virus candidate NK0238. </ItemContent></ListItem> <ListItem><ItemContent> • NK0238 exhibited a broad antivirus spectrum in greenhouse. </ItemContent></ListItem> <ListItem><ItemContent> • NK0238 showed comparable antivirus activities as controls in field trials. </ItemContent></ListItem> <ListItem><ItemContent> • NK0238 was safe to birds, fish, bees and silkworms. </ItemContent></ListItem> <ListItem><ItemContent> • NK0238 has a very good prospect in commercial development. </ItemContent></ListItem></List> It has previously been shown that tryptophan, the biosynthesis precursor of Peganum harmala alkaloids, and its derivatives have anti-TMV activity both in vitro and in vivo. Further exploration of this led to the identification of NK0238 as a highly effective agent for the prevention and control of diseases caused by plant viruses, but the existing routes are unsuitable for its large-scale synthesis. This study optimized a route for two-step synthesis of this virucide candidate via reaction of l-tryptophan with triphosgene to produce l-tryptophan-N-carboxylic anhydride, which then reacts with n-octylamine to give NK0238 at up to 94% yield and nearly 97% HPLC purity. In addition, the route was used for the preparation of NK0238 on a>40 g scale permitting further assessment of its antivirus activity in the greenhouse and field experiments, and toxicity tests. NK0238 exhibited useful antiviral activities against a variety of viruses both in greenhouse and field experiments. The toxicity tests showed that NK0238 was not acutely toxic to birds, fish, honey bees and silkworms. The optimized route provides a solid foundation for its large-scale synthesis and subsequent efficacy and toxicity studies, its excellent activity and safety make NK0238 a promising drug candidate for further development." @default.
- W4237217424 created "2022-05-12" @default.
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- W4237217424 date "2022-01-01" @default.
- W4237217424 modified "2023-10-17" @default.
- W4237217424 title "ROUTE DEVELOPMENT, ANTIVIRAL STUDIES, FIELD EVALUATION AND TOXICITY OF AN ANTIVIRAL PLANT PROTECTANT NK0238" @default.
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- W4237217424 doi "https://doi.org/10.15302/j-fase-2021390" @default.
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