Conti Cinzia, Proietti Monaco Luca, Desideri Nicoletta
Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Scienze di Sanità Pubblica, Sezione di Microbiologia, Sapienza-Università di Roma, P.le A. Moro, 5, 00185 Roma, Italy.
Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza-Università di Roma, P.le A. Moro, 00185 Roma, Italy.
Bioorg Med Chem. 2014 Feb 1;22(3):1201-7. doi: 10.1016/j.bmc.2013.11.054. Epub 2013 Dec 8.
Human rhinoviruses (HRVs) are the most common cause of viral respiratory infections and their complications. So far, no anti-viral agent has been approved for prevention or treatment of HRV infections. Pursuing our researches on small molecules with anti-rhinovirus activity, in this paper we describe the synthesis and in vitro anti-HRV 1B and 14 properties of new [2-(2H-chromen-3-yl)vinyl]pyridines and 3-[2-(pyridinyl)vinyl]-4H-chromen-4-ones. Generally, the synthesized compounds interfered with the replication of both serotypes at the micromolar or submicromolar concentrations. Preliminary results on their mechanism of action, performed on selected (E)-2-[2-(2H-chromen-3-yl)vinyl]pyridine, indicate an interference with the early step(s) of HRV 1B and 14 replication, probably at the uncoating level.
人鼻病毒(HRVs)是病毒性呼吸道感染及其并发症最常见的病因。到目前为止,尚无抗病毒药物被批准用于预防或治疗HRV感染。在对具有抗鼻病毒活性的小分子进行研究的过程中,本文描述了新型[2-(2H-色烯-3-基)乙烯基]吡啶和3-[2-(吡啶基)乙烯基]-4H-色烯-4-酮的合成及其体外抗HRV 1B和14的特性。一般来说,合成的化合物在微摩尔或亚微摩尔浓度下可干扰这两种血清型病毒的复制。对选定的(E)-2-[2-(2H-色烯-3-基)乙烯基]吡啶进行的作用机制初步研究表明,其可能在脱壳水平干扰HRV 1B和14复制的早期步骤。