| Literature DB >> 31003866 |
Yuki Okano1, Noriko Saito-Tarashima1, Madoka Kurosawa2, Ai Iwabu2, Masashi Ota1, Tadashi Watanabe2, Fumihiro Kato3, Takayuki Hishiki4, Masahiro Fujimuro5, Noriaki Minakawa6.
Abstract
In this work, we developed imidazole nucleoside derivatives with anti-dengue virus (DENV) activity was examined. First, compounds in a nucleosides library were screened to find lead compounds which inhibit replication of DENV. As a result, 5-ethynyl-(1-β-d-ribofuranosyl)imidazole-4-carboxamide (1; EICAR) and its 4-carbonitrile derivative EICNR (2) were selected as promising antiviral compounds. However, both of them also exhibited cytotoxicity. In order to develop an effective and less toxic compound, 4'-thio and 4'-seleno derivatives of EICAR and EICNR 3-6 were prepared. The resulting 4'-thioEICAR and 4'-thioEICNR showed inhibitory effect on DENV replication without cytotoxicity as potent as ribavirin, a positive control.Entities:
Keywords: 4′-Seleno-modification; 4′-Thio-modification; Antiviral activity; Dengue virus; Imidazole nucleoside
Year: 2019 PMID： 31003866 DOI： 10.1016/j.bmc.2019.04.015
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641