Abstract
Simple methods for synthesizing cis-4-guanidino-l-proline derivatives and 1-carbamimidoyl-l-proline derivatives as influenza neuraminidase inhibitors were developed. All of these compounds were prepared originally from l-hydroxyproline through a key intermediate. Among them, compound 4d with the scaffold of cis-4-guanidino-l-proline was the best inhibitor. The docking studies indicated that it could interact with the active site of NA similar to the binding pattern of peramivir. These compounds and the synthetic methods could be useful for exploration of novel influenza NA inhibitors.
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This work was supported by the 12th Five Years National Science and Technology Major Project of Ministry of Science and Technology of China (2011ZX09401-015) and Doctoral Fund of Ministry of Education of China (No. 20110131110037).
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Xie, Y., Xu, D., Wang, J. et al. Synthesis of cis-4-guanidino-l-proline and 1-carbamimidoyl-l-proline derivatives as influenza neuraminidase inhibitors. Med Chem Res 24, 1013–1017 (2015). https://doi.org/10.1007/s00044-014-1157-z
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DOI: https://doi.org/10.1007/s00044-014-1157-z