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In this paper, 18 novel chrysin derivatives were designed and synthesized. All target compounds were tested for anti-Toxoplasma activity by methyl thiazolyl tetrazolium (MTT) colorimetric method. The chemical structures were characterized by 1 H NMR, 13 C NMR and HRMS spectra. The selectivity index of 5-hydroxy-7-methoxy-4-oxo-N,2-diphenyl-4H-chromene-8-sulfonamide (D2) was 1.76, indicating that the anti-toxoplasma activity of compound D2 was significantly higher than that of the lead compound chrysin and the positive control drug sulfadiazine. Keywords chrysin derivatives; synthesis; toxoplasma activity; in vitro; selectivity index 弓形虫(Toxoplasma gondii

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Nineteen mycophenolic acid (MPA) derivatives were designed and synthesized, and their anti-Toxoplasma activity evaluated for the rst time. Among them, N-propylimidazole-modi ed compound E5 demonstrated the strongest activity, and the IC 50 against HFF-1 (Human Foreskin Fibroblasts-1) cells following infection with T. gondii is 80.9 μM (MPA-211.5 μM) and its selectivity value is 2.2 (MPA-1.2). In vivo experiments, E5 signi cantly inhibited the proliferation of tachyzoites in the abdominal cavity of mice acutely infected with T. gondii (inhibition rates 46.7%), and this inhibitory effect was greater than that of spiramycin (inhibition rates 31.3%) and MPA (inhibition rates 15.9%), this indicated that E5 had signi cant protective effects on the host during acute Toxoplasma infection. In addition E5 signi cantly reduced the levels of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) in the serum of infected mice, signi cantly increased the level of glutathione (GSH) in the liver, and signi cantly reduced the level of malondialdehyde (MDA), indicating that it has a signi cant hepatoprotective effect against T. gondii infection. Similarly, E5 can relieve hepatomegaly and splenomegaly induced by acute Toxoplasma infection. Spiramycin aggravated appetite loss in infected mice, while E5 did not. In summary, the results indicated that E5 has potential as a candidate anti-T. gondii drug.

Nineteen mycophenolic acid (MPA) derivatives were designed and synthesized, and their anti-Toxoplasma activity evaluated for the first time. Among them, N-propylimidazole-modified compound E5 demonstrated the strongest activity, and the IC50 against HFF-1 (Human Foreskin Fibroblasts-1) cells following infection with T. gondii is 80.9 μM (MPA-211.5 μM) and its selectivity value is 2.2 (MPA-1.2). In vivo experiments, E5 significantly inhibited the proliferation of tachyzoites in the abdominal cavity of mice acutely infected with T. gondii (inhibition rates 46.7%), and this inhibitory effect was greater than that of spiramycin (inhibition rates 31.3%) and MPA (inhibition rates 15.9%), this indicated that E5 had significant protective effects on the host during acute Toxoplasma infection. In addition E5 significantly reduced the levels of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) in the serum of infected mice, significantly increased the level of glutathione (GSH) in the liver, and significantly reduced the level of malondialdehyde (MDA), indicating that it has a significant hepatoprotective effect against T. gondii infection. Similarly, E5 can relieve hepatomegaly and splenomegaly induced by acute Toxoplasma infection. Spiramycin aggravated appetite loss in infected mice, while E5 did not. In summary, the results indicated that E5 has potential as a candidate anti-T. gondii drug.