Parasitic roundworms cause significant sickness and mortality in animals and humans. In livestock, these nematodes have severe economic impact and result in losses in food production on a global scale. None of the currently available drugs ideally suit all treatment circumstances, and the development of drug-resistant nematode strains has become a challenge to control the infection. There is an urgent need to develop novel anthelmintic compounds. According to our previous report, N-methylbenzo[d]oxazol-2-amine (1) showed anthelmintic activity and lowest cytotoxicity. In this study, in vivo anthelmintic properties were evaluated using Trichinella spiralis infected mice. Toxicity was evaluated using the rats and mode of action using molecular docking and metabolomics approaches. The in vivo results demonstrate that a dose of 250 mg/kg reduced the T. spiralis abundance in the digestive tract by 49%. The 250 mg/kg Albendazole was served as control. The relatively low acute toxicity was categorized into chemical category 5, with an LD₅₀ greater than 2000 mg/kg body. Molecular docking analysis showed the T. spiralis tubulin beta chain and glutamate-gated channels might not be the main targets of compound 1. Metabolomics analysis was used to explain the effects of compound 1 on the T. spiralis adult worm. The results demonstrated that compound 1 significantly up-regulated the metabolism of purine, pyrimidine and down-regulated sphingolipid metabolism. In conclusion, compound 1 could be a potential molecule for anthelmintic development. The bioavailability, pharmacokinetics, and absorption of this compound should be studied further to provide information for its future efficacy improvement.

寄生蛔虫会导致动物和人类严重疾病和死亡。对于牲畜来说，这些线虫具有严重的经济影响，并导致全球范围内的粮食生产损失。目前可用的药物没有一种能够理想地适合所有治疗情况，并且耐药线虫菌株的开发已成为控制感染的挑战。迫切需要开发新型驱虫化合物。根据我们之前的报告， N-甲基苯并[d]恶唑-2-胺 ( 1 ) 显示出驱虫活性和最低的细胞毒性。在这项研究中，使用旋毛虫感染的小鼠评估了体内驱虫特性。使用大鼠和分子对接和代谢组学方法的作用方式评估毒性。体内结果表明，250 mg/kg 的剂量使消化道中的旋毛虫丰度降低了 49%。 250mg/kg阿苯达唑作为对照。急性毒性较低，属于第5类化学物质，LD ₅₀大于2000 mg/kg体重。分子对接分析表明，螺旋毛虫微管蛋白β链和谷氨酸门控通道可能不是化合物1的主要靶标。使用代谢组学分析来解释化合物1对旋毛虫成虫的影响。结果表明，化合物1显着上调嘌呤、嘧啶代谢，下调鞘脂代谢。总之，化合物1可能是开发驱虫药的潜在分子。 应进一步研究该化合物的生物利用度、药代动力学和吸收，为其未来疗效的改进提供信息。