Synthesis and anti-rhinovirus activity of novel 3-[2-(pyridinyl)vinyl]substituted-2H-chromenes and-4H-chromen-4-ones

被引:31
作者
Conti, Cinzia [1 ]
Monaco, Luca Proietti [2 ]
Desideri, Nicoletta [2 ]
机构
[1] Univ Roma La Sapienza, Dipartimento Sci Sanita Pubbl, Ist Pasteur Fdn Cenci Bolognetti, Sez Microbiol, I-00185 Rome, Italy
[2] Univ Roma La Sapienza, Dipartimento Chim & Tecnol Farmaco, Ist Pasteur Fdn Cenci Bolognetti, I-00185 Rome, Italy
关键词
Chromenes; Chromen-4-ones; Pyridine derivatives; Rhinovirus; Antiviral activity; Capsid binders; AMIDINO-SUBSTITUTED FLAVANOIDS; 2H-CHROMENE DERIVATIVES; IN-VITRO; MECHANISM; RHINOVIRUSES; ISOFLAVANS; POLIOVIRUS; BINDING; TYPE-2; CYANO;
D O I
10.1016/j.bmc.2013.11.054
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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. (C) 2013 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1201 / 1207
页数:7
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