2. Academic Validation
  3. A new series of HAPs as anti-HBV agents targeting at capsid assembly

A new series of HAPs as anti-HBV agents targeting at capsid assembly

  • Bioorg Med Chem Lett. 2014 Sep 1;24(17):4247-9. doi: 10.1016/j.bmcl.2014.07.032.
Xiu-yan Yang 1,  Xiao-qian Xu 1,  Hua Guan 2,  Li-li Wang 3,  Qin Wu 4,  Guo-ming Zhao 5,  Song Li 1
Affiliations

Affiliations

  • 1 School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, PR China; Department of Medicinal Chemistry, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, PR China.
  • 2 Beijing Institute of Radiation Medicine, Beijing 100850, PR China.
  • 3 Department of Medicinal Chemistry, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, PR China.
  • 4 The Liver Cirrhosis Diagnosis and Treatment Centre, The 302 Military Hospital of China, Beijing 100039, PR China. Electronic address: [email protected].
  • 5 Department of Medicinal Chemistry, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, PR China. Electronic address: [email protected].
PMID: 25127104 DOI: 10.1016/j.bmcl.2014.07.032
Abstract

A series of novel Heteroaryldihydropyrimidines (HAPs) derivatives were designed and synthesized as potent inhibitors of HBV capsid assembly. These compounds were prepared from efforts to optimize an earlier series of HAPs, and compounds Mo1, Mo7, Mo8, Mo10, Mo12, and Mo13 demonstrated potent inhibition of HBV DNA replication at submicromolar range.

Keywords

Anti-HBV; Capsid; HAPs; SEC.

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