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N-((1,3-Diphenyl-1H-pyrazol-4-yl)methyl)anilines: A novel class of anti-RSV agents.

Authors :
Fioravanti R
Desideri N
Biava M
Droghini P
Atzori EM
Ibba C
Collu G
Sanna G
Delogu I
Loddo R
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2015 Jun 01; Vol. 25 (11), pp. 2401-4. Date of Electronic Publication: 2015 Apr 09.
Publication Year :
2015

Abstract

A series of N-((1,3-diphenyl-1H-pyrazol-4-yl)methyl)anilines were synthesized and evaluated in vitro for cytotoxicity and antiviral activity against a large panel of viruses. Most of the tested compounds interfered with RSV replication in the micromolar concentrations (EC50s ranging from 5 μM to 28 μM). SAR studies suggested that the presence of a trifluoromethyl group in R(1) abolished the anti-RSV activity and enhanced the cytotoxicity while the best results in term of both anti-RSV activity and selectivity were obtained by the introduction in R(1) of a chlorine or a bromine atom.<br /> (Copyright © 2015 Elsevier Ltd. All rights reserved.)

Details

Language :
English
ISSN :
1464-3405
Volume :
25
Issue :
11
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
25913116
Full Text :
https://doi.org/10.1016/j.bmcl.2015.04.006