title: Synthesis and biological evaluation of Matijing-Su derivatives as potent anti-HBV agents.
abstract: A series of Matijing-Su (MTS, N-(N-benzoyl-l-phenylalanyl)-O-acetyl-L-phenylalanol) derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity in 2.2.15 cells. The IC(50) of compounds 14a (0.71 μM), 13c (2.85 μM), 13b (4.37 μM), etc. and the selective index of 13g (161.01), 13c (90.45), 13a (85.09) etc. of the inhibition on the replication of HBV DNA were better than those of the positive control lamivudine (IC(50): 82.42 μM, SI: 41.59). Compounds 13o, 13p, and 16a also exhibited significant anti-HBV activity.
authors.affiliation: Center for Research and Development of Fine Chemicals of Guizhou University, Huaxi Road, Guiyang 550025, PR China.
authors.forename: Jingying
authors.initials: J
authors.lastname: Qiu
authors.forename: Bixue
authors.initials: B
authors.lastname: Xu
authors.forename: Zhengming
authors.initials: Z
authors.lastname: Huang
authors.forename: Weidong
authors.initials: W
authors.lastname: Pan
authors.forename: Peixue
authors.initials: P
authors.lastname: Cao
authors.forename: Changxiao
authors.initials: C
authors.lastname: Liu
authors.forename: Xiaojiang
authors.initials: X
authors.lastname: Hao
authors.forename: Baoan
authors.initials: B
authors.lastname: Song
authors.forename: Guangyi
authors.initials: G
authors.lastname: Liang
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D004151:Dipeptides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006515:Hepatitis B virus / Q000187:drug effects*; D006801:Humans; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014779:Virus Replication / Q000187:drug effects
chemical_list: D000998:Antiviral Agents; D004151:Dipeptides