Synthesis of acylguanidine zanamivir derivatives as neuraminidase inhibitors and the evaluation of their bio-activities

Chien Hung Lin; Tsung Che Chang; Anindya Das; Ming Yu Fang; Hui Chen Hung; Kai Cheng Hsu; Jinn Moon Yang; Mark Von Itzstein; Kwok Kong T. Mong; Tsu An Hsu; Chun Cheng Lin

doi:10.1039/c3ob40624e

Synthesis of acylguanidine zanamivir derivatives as neuraminidase inhibitors and the evaluation of their bio-activities

Chien Hung Lin, Tsung Che Chang, Anindya Das, Ming Yu Fang, Hui Chen Hung, Kai Cheng Hsu, Jinn Moon Yang, Mark Von Itzstein, Kwok Kong T. Mong, Tsu An Hsu, Chun Cheng Lin

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

32 Citations (Scopus)

Abstract

A series of acylguanidine-modified zanamivir analogs were synthesized and their inhibitory activities against the NAs of avian influenza viruses (H1N1 and H3N2) were evaluated. In particular, zanamivir derivative 3j, with a hydrophobic naphthalene substituent, exhibits the best inhibitory activity against group-1 NA with an IC₅₀ of 20 nM.

Original language	English
Pages (from-to)	3943-3948
Number of pages	6
Journal	Organic and Biomolecular Chemistry
Volume	11
Issue number	24
DOIs	https://doi.org/10.1039/c3ob40624e
Publication status	Published - Jun 28 2013
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Physical and Theoretical Chemistry
Organic Chemistry

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10.1039/c3ob40624e

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title = "Synthesis of acylguanidine zanamivir derivatives as neuraminidase inhibitors and the evaluation of their bio-activities",

abstract = "A series of acylguanidine-modified zanamivir analogs were synthesized and their inhibitory activities against the NAs of avian influenza viruses (H1N1 and H3N2) were evaluated. In particular, zanamivir derivative 3j, with a hydrophobic naphthalene substituent, exhibits the best inhibitory activity against group-1 NA with an IC50 of 20 nM.",

author = "Lin, {Chien Hung} and Chang, {Tsung Che} and Anindya Das and Fang, {Ming Yu} and Hung, {Hui Chen} and Hsu, {Kai Cheng} and Yang, {Jinn Moon} and {Von Itzstein}, Mark and Mong, {Kwok Kong T.} and Hsu, {Tsu An} and Lin, {Chun Cheng}",

year = "2013",

month = jun,

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doi = "10.1039/c3ob40624e",

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journal = "Organic and Biomolecular Chemistry",

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T1 - Synthesis of acylguanidine zanamivir derivatives as neuraminidase inhibitors and the evaluation of their bio-activities

AU - Lin, Chien Hung

AU - Chang, Tsung Che

AU - Das, Anindya

AU - Fang, Ming Yu

AU - Hung, Hui Chen

AU - Hsu, Kai Cheng

AU - Yang, Jinn Moon

AU - Von Itzstein, Mark

AU - Mong, Kwok Kong T.

AU - Hsu, Tsu An

AU - Lin, Chun Cheng

PY - 2013/6/28

Y1 - 2013/6/28

N2 - A series of acylguanidine-modified zanamivir analogs were synthesized and their inhibitory activities against the NAs of avian influenza viruses (H1N1 and H3N2) were evaluated. In particular, zanamivir derivative 3j, with a hydrophobic naphthalene substituent, exhibits the best inhibitory activity against group-1 NA with an IC50 of 20 nM.

AB - A series of acylguanidine-modified zanamivir analogs were synthesized and their inhibitory activities against the NAs of avian influenza viruses (H1N1 and H3N2) were evaluated. In particular, zanamivir derivative 3j, with a hydrophobic naphthalene substituent, exhibits the best inhibitory activity against group-1 NA with an IC50 of 20 nM.

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SP - 3943

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JO - Organic and Biomolecular Chemistry

JF - Organic and Biomolecular Chemistry

IS - 24

ER -

Synthesis of acylguanidine zanamivir derivatives as neuraminidase inhibitors and the evaluation of their bio-activities

Abstract

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