Rigid amphipathic fusion inhibitors are potent broad-spectrum antivirals based on the perylene scaffold, usually decorated with a hydrophylic group linked via ethynyl or triazole. We have sequentially simplified these structures by removing sugar moiety, then converting uridine to aniline, then moving to perylenylthiophenecarboxilic acids and to perylenylcarboxylic acid. All these polyaromatic compounds, as well as antibiotic heliomycin, still showed pronounced activity against tick-borne encephalitis virus (TBEV) with limited toxicity in porcine embryo kidney (PEK) cell line. 5-(Perylen-3-yl)-2-thiophenecarboxylic acid (5a) showed the highest antiviral activity with 50% effective concentration of approx. 1.6 nM.

刚性两亲性融合抑制剂是基于pot骨架的强效广谱抗病毒药物，通常用乙炔基或三唑连接的亲水基修饰。我们通过去除糖部分，然后将尿苷转化为苯胺，然后向过烯基噻吩羧酸和向过烯基羧酸转移，从而简化了这些结构。所有这些多环芳族化合物以及抗生素Heliomycin仍对tick传脑炎病毒（TBEV）表现出明显的活性，并且对猪胚胎肾（PEK）细胞系的毒性有限。5-（Perylen-3-yl）-2-thiophene羧酸（5a）显示最高的抗病毒活性，有效浓度约为50％。1.6 nM。