Advanced generation of paeonol-phenylsufonyl derivatives as potential anti-HBV agents

被引：8
|
作者：
Huang, Y. P. [1 ]
Shih, H. P. [1 ]
Liang, Y. C. [2 ]
Lin, H. H. [3 ]
Lin, M. C. [4 ]
Chen, C. W. [5 ,6 ]
Huang, T. J. [7 ]
Kuo, Y. C. [8 ]
Han, C. C. [1 ]
Hsu, M. H. [9 ,10 ]
机构：
[1] Natl Tsing Hua Univ, Dept Chem, Hsinchu 30013, Taiwan
[2] Acad Sinica, Agr Biotechnol Res Ctr, Taipei 115, Taiwan
[3] Taipei Vet Gen Hosp, Dept Oncol, Div Radiotherapy, Taipei 115, Taiwan
[4] Ind Technol Res Inst, Biomed Technol & Device Res Labs, Hsinchu 30013, Taiwan
[5] China Med Univ Hosp, Dept Anesthesiol, Taichung 404, Taiwan
[6] China Med Univ, Sch Med, Dept Anesthesiol, Taichung 404, Taiwan
[7] China Med Univ, Sch Med, Taichung 404, Taiwan
[8] Show Chwan Mem Hosp, Radiat Oncol, Changhua 50008, Taiwan
[9] Natl Tsing Hua Univ, Nucl Sci Technol Dept Ctr, Hsinchu 30013, Taiwan
[10] Tamkang Univ, Dept Chem, New Taipei 25137, Taiwan
来源：
RSC ADVANCES | 2016年 / 6卷 / 49期
关键词：
HEPATITIS-B; DISCOVERY; DESIGN;
D O I：
10.1039/c6ra06119b
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
Hepatitis B virus (HBV) infection causes serious liver diseases, and the development of effective drugs for chronic hepatitis B treatment remains an important step towards the eradication of HBV worldwide. Recently, our group designed paeonol-phenylsulfonyl derivatives and found that the compound 2-acetyl-5-methoxyphenyl 4-methoxybenzenesulfonate (6f) had the most potent antiviral effect against HBV, with an IC50 value of 0.36 mu M and a high selectivity index (SI; TC50/IC50) of 47.75. In this research, we modified compound 6f with a 2-aminothiazole scaffold and generated 13 novel paeonol derivatives by utilizing various benzoyl and acyl chlorides. Among this new generation, compound 2-(2-benzamidothiazol-4-yl)-5-methoxyphenyl 4-methoxybenzenesulfonate (8a) showed the highest SI value of 59.14 which exceeds those of compound 6f and lamivudine (3TC), a commercially available antiviral drug. Hence, we believe that our studies may offer some useful information for the development of antiviral medicines.
引用
收藏
页码：43556 / 43562
页数：7
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