• Patchliner

    兼顾科研与工业的全自动膜片钳系统
  • Patchliner

    自主生产与质量控制的耗材
  • Patchliner

    拥有超过10年实验设计与支持的经验
  • Dynamite8

    Automated Dynamic Clamp
  • Patchliner

    拥有所有手动膜片钳的特征与优点

2022 - Discovery of SHR5133, a Highly Potent and Novel HBV Capsid Assembly Modulator

icon pl Patchliner Publication in ACS Medicinal Chemistry Letters (2022)

Authors:
Li X., Zhang Z., Chen Y., Wang B., Yang G., Xu X., Yechao B., Bai D., Feng B., Mao Y., Feng J., Bai C., He F., Tao W.

Journal:
ACS Medicinal Chemistry Letters (2022) doi:10.1021/acsmedchemlett.2c00002


Abstract: 

Capsid assembly modulators (CpAMs) represent a new class of antivirals targeting hepatitis B virus (HBV) core protein to disrupt the assembly process. In this work, a novel chemotype featuring a fused heterocycle amide was discovered through pharmacophore exploration. Lead optimization resulted in compound 8 with an EC50 value of 511 nM, and then methyl substitution on the piperazine was found to improve the in vitro potency remarkably. Further SAR studies established the key compound SHR5133, which showed high in vitro antiviral potency, favorable pharmacokinetic profiles across species, and robust in vivo efficacy.


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