title: Synthesis and anti-hepatitis B virus activity of a novel class of thiazolylbenzimidazole derivatives.
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.
authors.affiliation: Department of Chemistry, East China Normal University, Shanghai, PR China.
authors.forename: Yu
authors.initials: Y
authors.lastname: Luo
authors.forename: Jia-Ping
authors.initials: JP
authors.lastname: Yao
authors.forename: Li
authors.initials: L
authors.lastname: Yang
authors.forename: Chun-Lan
authors.initials: CL
authors.lastname: Feng
authors.forename: Wei
authors.initials: W
authors.lastname: Tang
authors.forename: Gui-Feng
authors.initials: GF
authors.lastname: Wang
authors.forename: Jian-Pin
authors.initials: JP
authors.lastname: Zuo
authors.forename: Wei
authors.initials: W
authors.lastname: Lu
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D016923:Cell Death / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D056945:Hep G2 Cells / Q000187:drug effects; D006515:Hepatitis B virus / Q000187:drug effects*; D006801:Humans; D020128:Inhibitory Concentration 50; D008826:Microbial Sensitivity Tests / Q000379:methods; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000998:Antiviral Agents; D001562:Benzimidazoles