Agamennone Mariangela, Superti Fabiana
Department of Pharmacy, University "G. d'Annunzio" of Chieti-Pescara, Via dei Vestini 31, 66100 Chieti, Italy.
National Centre for Innovative Technologies in Public Health, National Institute of Health, Viale Regina Elena 299, 00161 Rome, Italy.
Pharmaceuticals (Basel). 2022 Feb 28;15(3):301. doi: 10.3390/ph15030301.
Influenza still represents a problematic disease, involving millions of people every year and causing hundreds of thousands of deaths. Only a few drugs are clinically available. The search for an effective weapon is still ongoing. In this scenario, we recently identified new drug-like compounds with antiviral activity toward two A/H1N1 Influenza virus strains, which were demonstrated to interfere with the processes mediated by hemagglutinin (HA). In the present work, the compound's ability to act against the A/H3N2 viral strain has been evaluated in hemagglutination inhibition (HI) assays. Two of the five tested compounds were also active toward the A/H3N2 Influenza virus. To validate the scaffold activity, analogue compounds of two broad-spectrum molecules were selected and purchased for HI testing on both A/H1N1 and A/H3N2 Influenza viruses. Forty-three compounds were tested, and four proved to be active toward all three viral strains. A computational study has been carried out to depict the HA binding process of the most interesting compounds.
流感仍然是一种棘手的疾病，每年感染数百万人并导致数十万人死亡。临床上可用的药物寥寥无几。寻找有效武器的工作仍在继续。在这种情况下，我们最近鉴定出了对两种甲型H1N1流感病毒株具有抗病毒活性的新型类药物化合物，这些化合物被证明可干扰血凝素（HA）介导的过程。在本研究中，通过血凝抑制（HI）试验评估了该化合物对甲型H3N2病毒株的作用能力。所测试的五种化合物中有两种对甲型H3N2流感病毒也具有活性。为了验证该骨架的活性，选择并购买了两种广谱分子的类似物进行针对甲型H1N1和甲型H3N2流感病毒的HI测试。测试了43种化合物，其中四种被证明对所有三种病毒株均具有活性。已开展一项计算研究来描述最具吸引力的化合物与HA的结合过程。
