INFLUENZA VIRUS NEURAMINIDASE INHIBITOR, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
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机译:流感病毒神经氨酸酶抑制剂,其制备方法及其应用
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摘要
The present invention relates to an influenza virus neuraminidase inhibitor, a preparation method therefor and an application thereof, which belong to the technical field of pharmaceutical chemistry. The structural general formula of the influenza virus neuraminidase inhibitor is shown in formula I, wherein: m is any natural number selected from 2-11, n is any natural number selected from 3-12, X is selected from OCOO or O; y is selected from formula aa, formula bb and formula cc; R in formula cc is selected from H or formula dd; R' in formula dd is H or a fluorescence labeling group; and Z is any natural number selected from 3-6. The described influenza virus neuraminidase inhibitor has significant inhibitory activity on various influenza viruses, especially on zanamivir-resistant influenza viruses (H3N2, E119V). The water solubility of an original medicine is remarkably improved, the lipid-water distribution coefficient is tens of times higher than that of the original medicine, and the inhibitor can be made into an oral preparation, which is a great breakthrough in pharmaceutical dosage forms.
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