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Synthesis and Anti-Hepatitis B Virus Activity of a Novel Class of Thiazolylbenzimidazole Derivatives

✍ Scribed by Yu Luo; Jia-Ping Yao; Li Yang; Chun-Lan Feng; Wei Tang; Gui-Feng Wang; Jian-Pin Zuo; Wei Lu

Publisher: John Wiley and Sons
Year: 2010
Tongue: English
Weight: 150 KB
Volume: 344
Category: Article
ISSN: 0365-6233
DOI: 10.1002/ardp.201000167

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✦ Synopsis

Abstract

Recently, heterocyclic benzimidazole derivatives have been investigated and validated as a promising class of antiviral agents. In this paper, a series of novel thiazolylbenzimidazole derivatives was synthesized and evaluated for their anti‐hepatitis B virus (HBV) activity and cytotoxicity on the HepG2.2.15 cell line. Afterwards, the preliminary structure–activity relationship (SAR) was discussed. Compound 8b, with IC~50~ = 1.1 µM and SI > 90.9, was the most promising compound and could be selected as a benchmark compound for further investigation.

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