| Autor: |
Xiaomeng He, Fan Wu, Wei Li, Runze Zhang, Ruiyang Sun, Zhihong Hu, Wu Zhong, Manli Wang |
| Jazyk: |
angličtina |
| Rok vydání: |
2024 |
| Předmět: |
|
| Zdroj: |
European Journal of Medicinal Chemistry Reports, Vol 12, Iss , Pp 100226- (2024) |
| Druh dokumentu: |
article |
| ISSN: |
2772-4174 |
| DOI: |
10.1016/j.ejmcr.2024.100226 |
| Popis: |
Favipiravir is a nucleobase analogue that exhibits antiviral activities against a variety of RNA viruses. Due to the lack of antivirals to combat SFTS, an emerging tickborne epidemic caused by a RNA virus belonging to the Phenuividae family within Bunyavirales, Favipiravir has been put brand new attention as optimal SFTS clinical candidate. We here disclose chemical synthesis of novel derivatives of Favipiravir. All derivatives showed favorable inhibitory effect on SFTSV replication in vitro. The 50 % effective concentration (EC50) of the most active compound H3 was 12.06 μM, better than that of Favipiravir (15.51 μM). Most importantly, compared with the clinical candidate Favipiravir, pharmacokinetic studies conducted on rats demonstrated enhanced pharmacokinetic properties for H2 and H3 including parameters of T1/2, Cmax and AUC. These combined attributes identified novel promising drug candidates for the treatment of SFTSV infection. |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
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