Department of Chemistry, Frontier Research Center on Fundamental and Applied Sciences of Matters, National Tsing Hua University, Hsinchu 300044, Taiwan.
Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium.
Int J Mol Sci. 2022 Oct 21;23(20):12675. doi: 10.3390/ijms232012675.
The yellow fever virus (YFV) is an emerging RNA virus and has caused large outbreaks in Africa and Central and South America. The virus is often transmitted through infected mosquitoes and spreads from area to area because of international travel. Being an acute viral hemorrhagic disease, yellow fever can be prevented by an effective, safe, and reliable vaccine, but not be eliminated. Currently, there is no antiviral drug available for its cure. Thus, two series of novel bis(benzofuran−1,3-imidazolidin-4-one)s and bis(benzofuran−1,3-benzimidazole)s were designed and synthesized for the development of anti-YFV lead candidates. Among 23 new bis-conjugated compounds, 4 of them inhibited YFV strain 17D (Stamaril) on Huh-7 cells in the cytopathic effect reduction assays. These conjugates exhibited the most compelling efficacy and selectivity with an EC50 of <3.54 μM and SI of >15.3. The results are valuable for the development of novel antiviral drug leads against emerging diseases.
黄热病病毒（YFV）是一种新兴的 RNA 病毒，已在非洲、中美洲和南美洲引发了大规模疫情。该病毒通常通过受感染的蚊子传播，并因国际旅行而在地区间传播。作为一种急性病毒性出血热，黄热病可以通过有效、安全和可靠的疫苗预防，但无法消除。目前，尚无针对该病毒的治疗方法的抗病毒药物。因此，为了开发抗 YFV 的先导候选药物，我们设计并合成了两个系列的新型双（苯并呋喃-1,3-咪唑烷-4-酮）和双（苯并呋喃-1,3-苯并咪唑）。在 23 种新的双共轭化合物中，有 4 种在细胞病变效应减少测定中抑制了在 Huh-7 细胞中的 YFV 株 17D（Stamaril）。这些共轭物表现出最引人注目的疗效和选择性，EC50<3.54 μM，SI>15.3。这些结果对于开发针对新兴疾病的新型抗病毒药物先导物具有重要价值。
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