Design and synthesis of pyridine-pyrazole-sulfonate derivatives as potential anti-HBV agents
| العنوان: | Design and synthesis of pyridine-pyrazole-sulfonate derivatives as potential anti-HBV agents |
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| المؤلفون: | Cheng Lin Yang, Tsurng Juhn Huang, Chia-Ching Chang, Lin Chiang Sherlock Huang, Jih Ru Hwu, Yi Jen Liao, Hong Chuang, Ming Hua Hsu, Chun Yi Wu, Mohit Kapoor |
| المصدر: | MedChemComm. 7:832-836 |
| بيانات النشر: | Royal Society of Chemistry (RSC), 2016. |
| سنة النشر: | 2016 |
| مصطلحات موضوعية: | 0301 basic medicine, Pharmacology, Hepatitis B virus, Drug, Stereochemistry, media_common.quotation_subject, Organic Chemistry, Pharmaceutical Science, Pyrazole, medicine.disease_cause, Biochemistry, High-performance liquid chromatography, 03 medical and health sciences, chemistry.chemical_compound, 030104 developmental biology, chemistry, Drug development, Drug Discovery, Pyridine, Gene expression, medicine, Molecular Medicine, IC50, media_common |
| الوصف: | Hepatitis B virus (HBV) is an infectious disease, which can cause acute and chronic infections. Every year, over 7.5 million persons die due to HBV. No effective drug exists for the treatment of HBV. Thus, we designed and synthesized 16 new pyridine-pyrazole-sulfonate compounds containing pyridine-SCH2-pyrazole and pyridine-pyrazole derivatives. Their structures were characterized by 1H-NMR, 13C-NMR, IR, mass spectroscopy, and high performance liquid chromatography. All the compounds were evaluated for their anti-HBV activities and a structure–activity relationship (SAR) in HepG2 2.2.15 cells was established. We found that the pyridine-pyrazole derivatives could inhibit the HBV gene expression and viral DNA replication. Among these compounds, 2-[3-(2-nitrophenylsulfonyl)oxy-5-pyrazol-yl]pyridine 19d has shown the most potent inhibitory activity with an IC50 value of 9.19 μM and high selectivity index, SI (TC50/IC50) of 35.46. Hence, we believe our compounds could serve as a potential lead compounds for anti-HBV drug development. |
| تدمد: | 2040-2511 2040-2503 |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=doi_________::3db7ac73c4640615c4813efdd826caf3Test https://doi.org/10.1039/c6md00008hTest |
| رقم الانضمام: | edsair.doi...........3db7ac73c4640615c4813efdd826caf3 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 20402511 20402503 |
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