1472003-80-7Relevant academic research and scientific papers
Design, synthesis, and evaluation of novel heteroaryldihydropyrimidine derivatives as non-nucleoside hepatitis B virus inhibitors by exploring the solvent-exposed region
Desta, Samuel,Ding, Xiao,Guo, Xiaowei,Jia, Haiyong,Liang, Xiaohong,Liu, Xinyong,Yu, Ji,Zhan, Peng,Zhang, Jian,Zhang, Shuo
, (2020)
In continuation of our efforts toward the discovery of potent non-nucleoside hepatitis B virus (HBV) inhibitors with novel structures, we have explored the solvent-exposed protein region of heteroaryldihydropyrimidine derivatives. Herein, the morpholine ring of GLS4 was replaced with substituted sulfonamides and triazoles to generate novel non-nucleoside HBV inhibitors with desirable potency. In in vitro biological evaluation, several derivatives showed good anti-HBV DNA replication activity compared to lamivudine. In particular, compound II-1 displayed the most potent activity against HBV DNA replication (IC50?=?0.35?±?0.04?μM). The preliminary structure–activity relationships of the new compounds were summarized, which may help in discovering more potent anti-HBV agents via rational drug design.
Dihydropyrimidine-sulfonamide derivative and preparation method and application thereof
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, (2019/01/06)
The invention discloses a dihydropyrimidine-sulfonamide derivative and a preparation method and an application thereof. The compound has a structure shown in a formula I. The invention further relatesto the preparation method of the compound containing the structure of the formula I and a pharmaceutical composition, and provides the application of the compound in preparation of an anti-HBV drug.
