期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 11, 页码 2938-2940出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.04.067
关键词
Ester prodrug; CS-8958; Zanamivir; Influenza; Long-acting NA inhibitor
A series of ester prodrugs of 7-O-methyl derivative of Zanamivir (compound 3) was synthesized and their efficacy was evaluated in an influenza infected mice model by intranasal administration. Compound 7c (CS-8958), octanoyl ester prodrug of the C-9 alcohol of compound 3, was found to be much longer-acting than Zanamivir. Furthermore, the in vivo efficacies of compounds 12a, 12b, and 12c, the linear alkyl ester prodrug of the carboxylic acid, were comparable to that exerted by compound 7c. (C) 2009 Published by Elsevier Ltd.
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