Discovery of the first series of small molecule H5N1 entry inhibitors

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

doi:10.1021/jm900275m

Discovery of the first series of small molecule H5N1 entry inhibitors

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

Research output: Contribution to journal › Article › peer-review

63 Scopus citations

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.

Original language	English
Pages (from-to)	7368-7371
Number of pages	4
Journal	Journal of Medicinal Chemistry
Volume	52
Issue number	23
DOIs	https://doi.org/10.1021/jm900275m
State	Published - 10 Dec 2009
Externally published	Yes

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title = "Discovery of the first series of small molecule H5N1 entry inhibitors",

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 = "Gaopeng Song and Sen Yang and Wei Zhang and Yingli Cao and Peng Wang and Ning Ding and Zaihong Zhang and Ying Guo and Yingxia Li",

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T1 - Discovery of the first series of small molecule H5N1 entry inhibitors

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 - 2009/12/10

Y1 - 2009/12/10

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.

AB - 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.

UR - http://www.scopus.com/inward/record.url?scp=72249102363&partnerID=8YFLogxK

U2 - 10.1021/jm900275m

DO - 10.1021/jm900275m

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VL - 52

SP - 7368

EP - 7371

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 23

ER -

Discovery of the first series of small molecule H5N1 entry inhibitors

Abstract

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