title: Identification of 1-isopropylsulfonyl-2-amine benzimidazoles as a new class of inhibitors of hepatitis B virus.
abstract: A series of 1-isopropylsulfonyl-2-amine benzimidazole derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. In general, these derivatives are potent HBV inhibitors (IC(50)<4 microM) with high selectivity indices (SIs>40). Compounds 5b-e, g, j, and 9a were among the most prominent compounds, with IC(50)s of 0.70-2.0 microM and SIs of 41-274. The potent anti-HBV activity and safety profiles of the most promising compounds 5d and j (IC(50)s=0.70 microM, SIs>120) demonstrate the potential of this series of benzimidazoles for the development of new anti-HBV drugs.
authors.affiliation: Institute of Medicinal Chemistry, Shanghai Key Laboratory of Green Chemistry and Chemical Process, Department of Chemistry, East China Normal University, 3663 North Zhongshan Road, Shanghai, Shanghai 200062, China.
authors.forename: Yun-Fei
authors.initials: YF
authors.lastname: Li
authors.forename: Gui-Feng
authors.initials: GF
authors.lastname: Wang
authors.forename: Yu
authors.initials: Y
authors.lastname: Luo
authors.forename: Wei-Gang
authors.initials: WG
authors.lastname: Huang
authors.forename: Wei
authors.initials: W
authors.lastname: Tang
authors.forename: Chun-Lan
authors.initials: CL
authors.lastname: Feng
authors.forename: Li-Ping
authors.initials: LP
authors.lastname: Shi
authors.forename: Yu-Dan
authors.initials: YD
authors.lastname: Ren
authors.forename: Jian-Ping
authors.initials: JP
authors.lastname: Zuo
authors.forename: Wei
authors.initials: W
authors.lastname: Lu
mesh_terms: D000818:Animals; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D002417:Cattle; D016923:Cell Death / Q000187:drug effects; D045744:Cell Line, Tumor; D004279:DNA, Viral / Q000096:biosynthesis; D006515:Hepatitis B virus / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D020128:Inhibitory Concentration 50
chemical_list: D001562:Benzimidazoles; D004279:DNA, Viral; C031000:benzimidazole