共 32 条
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.
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页码:1201 / 1207
页数:7
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