Design and synthesis of novel benzimidazole derivatives as inhibitors of hepatitis B virus.
A series of novel benzimidazole derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. The preliminary SAR was discussed. Compound 12a, with IC50<0.41 microM and SI>81.2, was the most promising compound and selected as the benchmark compound for further optimization.
Luo
Yu
Y
Department of Chemistry, East China Normal University, 3663 North Zhongshan Road, Shanghai 200062, PR China.
Yao
Jia-Ping
JP
Yang
Li
L
Feng
Chun-Lan
CL
Tang
Wei
W
Wang
Gui-Feng
GF
Zuo
Jian-Pin
JP
Lu
Wei
W
D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D006509:Hepatitis B / Q000188:drug therapy*; D006515:Hepatitis B virus / Q000187:drug effects*; D006801:Humans; D013329:Structure-Activity Relationship
D000998:Antiviral Agents; D001562:Benzimidazoles