Discovery of the First Series of Small Molecule H5N1 Entry Inhibitors Export

by: Gaopeng Song, Sen Yang, Wei Zhang, Yingli Cao, Peng Wang, Ning Ding, Zaihong Zhang, Ying Guo, Yingxia Li

Journal of Medicinal Chemistry, Vol. 0, No. 0. (0000)

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Abstract

The occurrence of highly pathogenic avian influenza virus H5N1 highlights the urgent need for new classes of antiviral drugs. Inhibition of H5N1 entry into cells may be an effective strategy. We report the first three small molecule inhibitors saponins with 3-O-β-chacotriosyl residue, which showed potent inhibitory activity with IC50 of 7.22−9.25 μM. The subsequent SAR studies showed the 3-O-β-chacotriosyl residue was essential for the activity, and the aglycone structure also affected the activity.

@article{citeulike:4920940, abstract = {The occurrence of highly pathogenic avian influenza virus H5N1 highlights the urgent need for new classes of antiviral drugs. Inhibition of H5N1 entry into cells may be an effective strategy. We report the first three small molecule inhibitors saponins with 3-O-β-chacotriosyl residue, which showed potent inhibitory activity with IC50 of 7.22−9.25 μM. The subsequent SAR studies showed the 3-O-β-chacotriosyl residue was essential for the activity, and the aglycone structure also affected the activity.}, author = {Song, Gaopeng and Yang, Sen and Zhang, Wei and Cao, Yingli and Wang, Peng and Ding, Ning and Zhang, Zaihong and Guo, Ying and Li, Yingxia}, citeulike-article-id = {4920940}, citeulike-linkout-0 = {http://dx.doi.org/10.1021/jm900275m}, citeulike-linkout-1 = {http://pubs.acs.org/doi/abs/10.1021/jm900275m}, doi = {10.1021/jm900275m}, journal = {Journal of Medicinal Chemistry}, keywords = {influenza}, number = {0}, posted-at = {2009-06-22 07:41:53}, priority = {2}, title = {Discovery of the First Series of Small Molecule H5N1 Entry Inhibitors}, url = {http://dx.doi.org/10.1021/jm900275m}, volume = {0}, year = {0000} }

RIS record

TY - JOUR ID - citeulike:4920940 L3 - citeulike-article-id:4920940 N2 - The occurrence of highly pathogenic avian influenza virus H5N1 highlights the urgent need for new classes of antiviral drugs. Inhibition of H5N1 entry into cells may be an effective strategy. We report the first three small molecule inhibitors saponins with 3-O-β-chacotriosyl residue, which showed potent inhibitory activity with IC50 of 7.22−9.25 μM. The subsequent SAR studies showed the 3-O-β-chacotriosyl residue was essential for the activity, and the aglycone structure also affected the activity. IS - 0 JF - Journal of Medicinal Chemistry TI - Discovery of the First Series of Small Molecule H5N1 Entry Inhibitors VL - 0 KW - influenza AU - Song, Gaopeng AU - Yang, Sen AU - Zhang, Wei AU - Cao, Yingli AU - Wang, Peng AU - Ding, Ning AU - Zhang, Zaihong AU - Guo, Ying AU - Li, Yingxia PY - 2000/// UR - http://dx.doi.org/10.1021/jm900275m ER -

Discovery of the First Series of Small Molecule H5N1 Entry Inhibitors Export

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