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  • Title: Synthesis and anti-hepatitis B virus activity of a novel class of thiazolylbenzimidazole derivatives.
    Author: Luo Y, Yao JP, Yang L, Feng CL, Tang W, Wang GF, Zuo JP, Lu W.
    Journal: Arch Pharm (Weinheim); 2011 Feb; 344(2):78-83. PubMed ID: 21290423.
    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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