ROUTE DEVELOPMENT,ANTIVIRAL STUDIES,FIELD EVALUATION AND TOXICITY OF AN ANTIVIRAL PLANT PROTECTANT NK0238 |
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| Authors: | Wentao XU Hao TIAN Hongjian SONG Yuxiu LIU Yongqiang LI Qingmin WANG |
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| Affiliation: | 1. State Key Laboratory of Elemento-Organic Chemistry, Research Institute of Elemento-Organic Chemistry, College of Chemistry, Nankai University, Tianjin 300071, China.2. Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), Tianjin 300071, China. |
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| Abstract: | ![]()
• Developed a two-step synthetic route to anti-plant-virus candidate NK0238. • NK0238 exhibited a broad antivirus spectrum in greenhouse. • NK0238 showed comparable antivirus activities as controls in field trials. • NK0238 was safe to birds, fish, bees and silkworms. • NK0238 has a very good prospect in commercial development. 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. |
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| Keywords: | antiviral plant protectant antiviral in the greenhouse field evaluation l-trp-NCA synthesis optimization toxicity tests |
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