57515-98-7Relevant academic research and scientific papers
Synthesis and evaluation of new phenyl acrylamide derivatives as potent non-nucleoside anti-HBV agents
Gu, Xiaoke,Zhang, Yinpeng,Zou, Yueting,Li, Xin,Guan, Mingyu,Zhou, Qingqing,Qiu, Jingying
, (2020/12/09)
As a continuation of our previous work, a series of new phenyl acrylamide derivatives (4Aa-g, 4Ba-t, 5 and 6a-c) were designed and synthesized as non-nucleoside anti-HBV agents. Among them, compound 4Bs could potently inhibit HBV DNA replication in wild-type and lamivudine (3TC)/entecavir resistant HBV mutant strains with IC50 values of 0.19 and 0.18 μM, respectively. Notably, the selective index value of 4Bs was above 526, indicating the favorable safety profile. Interestingly, unlike nucleoside analogue 3TC, 4Bs could significantly inhibit 3.5 kb pgRNA expression. Molecular docking study revealed that 4Bs could fit well into the dimer-dimer interface of HBV core protein by hydrophobic, π–π and H-bond interactions. Considering the potent anti-HBV activity, low toxicity and diverse anti-HBV mechanism from that of nucleoside anti-HBV agent 3TC, compound 4Bs might be a promising lead to develop novel non-nucleoside anti-HBV therapeutic agents, and warranted further investigation.
Electrochemical Reactions. Part 24. Reductive Cyclisation of i-(2-Halogenophenyl)-j-phenyl Compounds: A General Reaction
Grimshaw, James,Hamilton, Robert,Trocha-Grimshaw, Jadwiga
, p. 229 - 234 (2007/10/02)
The phenyl ?-radical formed by reduction of aryl halides in an aprotic solvent undergoes efficient radical substitution on an adjacent benzene ring.Several examples of this cyclisation reaction are given.The reaction is appropriate for the synthesis of 6-membered aromatic rings where the two reacting phenyl groups are held in a cis-configuration by an olefin bond or another aromatic ring.
