当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Synthesis, biological activity and structure-activity relationship of 4,5-dimethoxybenzene derivatives inhibitor of rhinovirus 14 infection.

Synthesis, biological activity and structure-activity relationship of 4,5-dimethoxybenzene derivatives inhibitor of rhinovirus 14 infection.

Abstract：

:Human rhinoviruses are a common cause of respiratory infections, and thus constitute an important target for medicinal chemistry. Still, no drug has been approved for clinical use. We report herein the discovery of dibenzenic derivatives with potent and specific in vitro anti-rhinoviral 14 activity. A total of 99 structural analogues were synthesized by an original synthesis method, i.e. through one organic agent Tetrakis(DimethylAmino)Ethylene (TDAE) and a structure-activity relationship was established. It was shown that 4,5-dimethoxy scaffold and the presence of a C-4 substituted aromatic moiety were necessary to the in vitro activity of these original agents. However, modifications on liker were not convincing. The benzonitrile derivative 23 was identified as the most potent and selective inhibitor of rhinovirus replication in these series (EC₅₀ of 2 ± 0.5 μM, CC₅₀ of 184 μM, selectivity index of 92).

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Roche M,Lacroix C,Khoumeri O,Franco D,Neyts J,Terme T,Leyssen P,Vanelle P

doi

10.1016/j.ejmech.2014.01.034

subject

Has Abstract

pub_date

2014-04-09 00:00:00

pages

445-59

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(14)00080-4

journal_volume

76

pub_type

杂志文章

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