Design, Synthesis, and Biological Evaluation of Novel Trifluoromethylated Dipeptide Mimetics of Matijin‐Su as Potent Anti‐HBV Agents
A series of Matijin-Su (MTS) derivatives were designed, synthesized and their anti-hepatitis B virus (HBV) activities were evaluated in vitro. Twelve compounds displayed good inhibitory activity against HBV DNA replication with IC<sub>50</sub> values at micromolar level (0.14-4.81 µM), and among them, compounds 13d, 13n, and 13o were selected for further study. Compound 13d suppressed the HBeAg secretion with IC<sub>50</sub> value of 2.57 µM (SI = 4.31), while had no effect on HBsAg. However, compounds 13n and 13o showed no effect to both HBeAg and HBsAg. The molecular docking studies indicated that compound 13d could form H-bond interaction with protein residues of HBV core protein which deserves further study.
Authors
- Anna A. Kuang
- Bixue Xu (ORCID: https://orcid.org/0000-0002-0388-2104)
- Xueling Meng (ORCID: https://orcid.org/0009-0009-8887-6122)
- Xiaoping Zeng (ORCID: https://orcid.org/0000-0002-9083-3860)
- Xiangkai Kong (ORCID: https://orcid.org/0000-0002-0552-5557)
- Xueling Shao
- Gang Yu (ORCID: https://orcid.org/0000-0002-8136-2307)
- Guangcan Xu
Institutions
- Guiyang College of Traditional Chinese Medicine (CN)
- Guiyang Medical University (CN)
- Guizhou University (CN)
- Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences (CN)
Publication Details
- Journal
- Chemistry & Biodiversity
- Published
- 2024-12-23
- DOI
- https://doi.org/10.1002/cbdv.202402061
- Primary Topic
- Hepatitis B Virus Studies
- Type
- article
- Field-Weighted Citation Impact
- 0.00