Design, Synthesis and Pharmacological Activity Testing of the Novel Neuraminidase Inhibitor

OBJECTIVE To design, synthesis novel neuraminidase inhibitors and detect their pharmacological activity for inhibite virus. METHODS The antiviral acyl thiourea fragments were integrated with the benzoic acid structure of neuraminidase inhibitors. Based on the pro-drug principle, 28 compounds were designed and synthesized and conduct the pharmacological activity screening. A/FM/1/47 (H1N1) strain was selected for the pharmacological activity test, and the single concentration(10 µmol·L^-1) inhibition rate of neuraminidase and in vitro virus inhibition test were performed respectively. RESULTS The results showed that I-2, I-5, I-11 and I-12 had desirable virus inhibitory activity, I-11 was the best among them. The virus inhibition rate of compound I-11 could reach 70.50%, which was superior to oseltamivir. CONCLUSION Preliminary study on structure-activity relationship of these 28 compounds will provide a basis for the design of the new neuraminidase inhibitors in the following study.