Academic Journal
Design, Synthesis and Discovery of N,N'-Carbazoyl-aryl-urea Inhibitors of Zika NS5 Methyltransferase and Virus Replication
| العنوان: | Design, Synthesis and Discovery of N,N'-Carbazoyl-aryl-urea Inhibitors of Zika NS5 Methyltransferase and Virus Replication |
|---|---|
| المؤلفون: | Spizzichino, S, Mattedi, G, Lauder, K, Valle, C, Aouadi, W, Canard, B, Decroly, E, Kaptein, SJF, Neyts, J, Graham, C, Sule, Z, Barlow, DJ, Silvestri, R, Castagnolo, D |
| المصدر: | ChemMedChem , 15 (4) pp. 385-390. (2020) |
| بيانات النشر: | WILEY-V C H VERLAG GMBH |
| سنة النشر: | 2020 |
| المجموعة: | University College London: UCL Discovery |
| مصطلحات موضوعية: | Science & Technology, Life Sciences & Biomedicine, Chemistry, Medicinal, Pharmacology & Pharmacy, Zika, flavivirus, methyltransferase, antiviral agents, urea, SMALL-MOLECULE INHIBITORS, DENGUE VIRUS, IDENTIFICATION, PROTEASE, INFECTION |
| الوصف: | The recent outbreaks of Zika virus (ZIKV) infection worldwide make the discovery of novel antivirals against flaviviruses a research priority. This work describes the identification of novel inhibitors of ZIKV through a structure‐based virtual screening approach using the ZIKV NS5‐MTase. A novel series of molecules with a carbazoyl‐aryl‐urea structure has been discovered and a library of analogues has been synthesized. The new compounds inhibit ZIKV MTase with IC50 between 23–48 μM. In addition, carbazoyl‐aryl‐ureas also proved to inhibit ZIKV replication activity at micromolar concentration. |
| نوع الوثيقة: | article in journal/newspaper |
| وصف الملف: | text |
| اللغة: | English |
| Relation: | https://discovery.ucl.ac.uk/id/eprint/10114105/1/cmdc.201900533.pdf; https://discovery.ucl.ac.uk/id/eprint/10114105/ |
| الاتاحة: | https://discovery.ucl.ac.uk/id/eprint/10114105/1/cmdc.201900533.pdf https://discovery.ucl.ac.uk/id/eprint/10114105/ |
| Rights: | open |
| رقم الانضمام: | edsbas.562B4451 |
| قاعدة البيانات: | BASE |
| الوصف غير متاح. |