Synthesis and anti-hepatitis B virus activity of novel benzimidazole derivatives

Yun Fei Li; Gui Feng Wang; Pei Lan He; Wei Gang Huang; Feng Hua Zhu; He Yong Gao; Wei Tang; Yu Luo; Chun Lan Feng; Li Ping Shi; Yu Dan Ren; Wei Lu; Jian Ping Zuo

doi:10.1021/jm060330f

Synthesis and anti-hepatitis B virus activity of novel benzimidazole derivatives

Yun Fei Li, Gui Feng Wang, Pei Lan He, Wei Gang Huang, Feng Hua Zhu, He Yong Gao, Wei Tang, Yu Luo, Chun Lan Feng, Li Ping Shi, Yu Dan Ren, Wei Lu^*, Jian Ping Zuo

^*Corresponding author for this work

School of Chemistry and Molecular Engineering

CAS - Shanghai Institute of Materia Medica

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

168 Scopus citations

Abstract

A series of novel benzimidazole derivatives was synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in vitro. Strong activity against HBV replication and low cytotoxicity were generally observed in these benzimidazoles. The most promising compounds were 12a and 12b, with similar high antiviral potency (IC₅₀ = 0.9 and 0.7 μM, respectively) and remarkable selectivity indices (> 1111 and 714, respectively). They were selected for further evaluation as novel HBV inhibitors.

Original language	English
Pages (from-to)	4790-4794
Number of pages	5
Journal	Journal of Medicinal Chemistry
Volume	49
Issue number	15
DOIs	https://doi.org/10.1021/jm060330f
State	Published - 27 Jul 2006

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10.1021/jm060330f

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@article{429fead09ffe4b71b78353c99eb1c2c0,

title = "Synthesis and anti-hepatitis B virus activity of novel benzimidazole derivatives",

abstract = "A series of novel benzimidazole derivatives was synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in vitro. Strong activity against HBV replication and low cytotoxicity were generally observed in these benzimidazoles. The most promising compounds were 12a and 12b, with similar high antiviral potency (IC50 = 0.9 and 0.7 μM, respectively) and remarkable selectivity indices (> 1111 and 714, respectively). They were selected for further evaluation as novel HBV inhibitors.",

author = "Li, \{Yun Fei\} and Wang, \{Gui Feng\} and He, \{Pei Lan\} and Huang, \{Wei Gang\} and Zhu, \{Feng Hua\} and Gao, \{He Yong\} and Wei Tang and Yu Luo and Feng, \{Chun Lan\} and Shi, \{Li Ping\} and Ren, \{Yu Dan\} and Wei Lu and Zuo, \{Jian Ping\}",

year = "2006",

month = jul,

day = "27",

doi = "10.1021/jm060330f",

language = "英语",

volume = "49",

pages = "4790--4794",

journal = "Journal of Medicinal Chemistry",

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publisher = "American Chemical Society",

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TY - JOUR

T1 - Synthesis and anti-hepatitis B virus activity of novel benzimidazole derivatives

AU - Li, Yun Fei

AU - Wang, Gui Feng

AU - He, Pei Lan

AU - Huang, Wei Gang

AU - Zhu, Feng Hua

AU - Gao, He Yong

AU - Tang, Wei

AU - Luo, Yu

AU - Feng, Chun Lan

AU - Shi, Li Ping

AU - Ren, Yu Dan

AU - Lu, Wei

AU - Zuo, Jian Ping

PY - 2006/7/27

Y1 - 2006/7/27

N2 - A series of novel benzimidazole derivatives was synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in vitro. Strong activity against HBV replication and low cytotoxicity were generally observed in these benzimidazoles. The most promising compounds were 12a and 12b, with similar high antiviral potency (IC50 = 0.9 and 0.7 μM, respectively) and remarkable selectivity indices (> 1111 and 714, respectively). They were selected for further evaluation as novel HBV inhibitors.

AB - A series of novel benzimidazole derivatives was synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in vitro. Strong activity against HBV replication and low cytotoxicity were generally observed in these benzimidazoles. The most promising compounds were 12a and 12b, with similar high antiviral potency (IC50 = 0.9 and 0.7 μM, respectively) and remarkable selectivity indices (> 1111 and 714, respectively). They were selected for further evaluation as novel HBV inhibitors.

UR - https://www.scopus.com/pages/publications/33746741042

U2 - 10.1021/jm060330f

DO - 10.1021/jm060330f

M3 - 文章

C2 - 16854087

AN - SCOPUS:33746741042

SN - 0022-2623

VL - 49

SP - 4790

EP - 4794

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 15

ER -

Synthesis and anti-hepatitis B virus activity of novel benzimidazole derivatives

Abstract

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