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Synthesis, biological activity and structure–activity relationship of 4,5-dimethoxybenzene derivatives inhibitor of rhinovirus 14 infection.
- Source :
-
European Journal of Medicinal Chemistry . Apr2014, Vol. 76, p445-459. 15p. - Publication Year :
- 2014
-
Abstract
- 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). [Copyright &y& Elsevier]
Details
- Language :
- English
- ISSN :
- 02235234
- Volume :
- 76
- Database :
- Academic Search Index
- Journal :
- European Journal of Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 95018229
- Full Text :
- https://doi.org/10.1016/j.ejmech.2014.01.034