title: A new series of HAPs as anti-HBV agents targeting at capsid assembly.
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.
authors.affiliation: 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.
authors.forename: Xiu-yan
authors.initials: XY
authors.lastname: Yang
authors.affiliation: 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.
authors.forename: Xiao-qian
authors.initials: XQ
authors.lastname: Xu
authors.affiliation: Beijing Institute of Radiation Medicine, Beijing 100850, PR China.
authors.forename: Hua
authors.initials: H
authors.lastname: Guan
authors.affiliation: Department of Medicinal Chemistry, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, PR China.
authors.forename: Li-li
authors.initials: LL
authors.lastname: Wang
authors.affiliation: The Liver Cirrhosis Diagnosis and Treatment Centre, The 302 Military Hospital of China, Beijing 100039, PR China. Electronic address: wuqin6@126.com.
authors.forename: Qin
authors.initials: Q
authors.lastname: Wu
authors.affiliation: Department of Medicinal Chemistry, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, PR China. Electronic address: zhaogm@bmi.ac.cn.
authors.forename: Guo-ming
authors.initials: GM
authors.lastname: Zhao
authors.affiliation: 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.
authors.forename: Song
authors.initials: S
authors.lastname: Li
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002213:Capsid / Q000187:drug effects* / Q000378:metabolism; D002470:Cell Survival / Q000187:drug effects; D004279:DNA, Viral / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D056945:Hep G2 Cells; D006515:Hepatitis B virus / Q000187:drug effects* / Q000254:growth & development; D006801:Humans; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014779:Virus Replication / Q000187:drug effects
chemical_list: D000998:Antiviral Agents; D004279:DNA, Viral; D011743:Pyrimidines
keywords: Anti-HBV; Capsid; HAPs; SEC