Design, Synthesis and Evaluation of Novel 4-(4-Chlorobenzyl)-6-methylpyridazin-3(2H)-one Derivatives as Hepatitis B Virus Inhibitors

被引：0
作者：
Tan, Oya Unsal [1 ]
Moncol, Jan [2 ]
Durantel, David [3 ,4 ]
机构：
[1] Hacettepe Univ, Fac Pharm, Dept Pharmaceut Chem, Ankara, Turkey
[2] Slovak Univ Technol Bratislava, Fac Chem & Food Technol, Dept Inorgan Chem, Bratislava, Slovakia
[3] Univ Lyon UCBL1, INSERM, U1052, Canc Res Ctr Lyon CRCL,CNRS UMR 5286,Ctr Leon Ber, F-69008 Lyon, France
[4] Univ Lyon UCBL1, INSERM, U1111, Int Ctr Infectiol Res CIRI,CNRS UMR 5308, Lyon, France
来源：
CHEMISTRYSELECT | 2022年 / 7卷 / 40期
关键词：
Anti-Hepatitis B virus activity; capsid assembly modulators; pyridazin-3-one; synthesis; x-ray analysis; NS5B POLYMERASE INHIBITORS; OPTIMIZATION; THIADIAZIN-3'-YL)-5-HYDROXY-2H-PYRIDAZIN-3-ONES; PYRIDAZIN-3(2H)-ONES; REPLICATION;
D O I：
10.1002/slct.202203164
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
22 Novel pyridazin-3-ones have been designed for anti-hepatitis B virus (HBV) activity by structural modifications of 3711 which is capsid assembly modulator. Structure of the target compounds were confirmed by elemental analysis and spectroscopic data including X-ray studies. Among them, the compound having piperazine moiety showed notable inhibitory activity on secretion of HBV DNA and HBeAg which is comparable to that of AT-130. The preliminary structure-activity relationships (SARs) of the newly synthesized pyridazin-3-one analogues were summarized, which may help researchers to discover more potent anti-HBV agents bearing pyridazine-3-one scaffold.
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页数：11
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