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 lM to 28 lM). SAR studies suggested that the presence of a trifluoromethyl group in R1 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 R1 of a chlorine or a bromine atom.

N-((1,3-diphenyl-1H-pyrazol-4-yl)methyl)anilines: a novel class of anti-RSV agents / Fioravanti, Rossella; Desideri, Nicoletta; Biava, Mariangela; Droghini, P.; Atzori, ELENA MARIA; Ibba, C.; Collu, G.; Sanna, G.; Delogu, I.; Loddo, R.. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - STAMPA. - 25:11(2015), pp. 2401-2404. [10.1016/j.bmcl.2015.04.006]

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

FIORAVANTI, Rossella;DESIDERI, Nicoletta;BIAVA, Mariangela;ATZORI, ELENA MARIA;
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 lM to 28 lM). SAR studies suggested that the presence of a trifluoromethyl group in R1 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 R1 of a chlorine or a bromine atom.
2015
pyrazole derivatives; aniline derivatives; antiviral activity; anti-RSV activity; RNA and DNA viruses
01 Pubblicazione su rivista::01a Articolo in rivista
N-((1,3-diphenyl-1H-pyrazol-4-yl)methyl)anilines: a novel class of anti-RSV agents / Fioravanti, Rossella; Desideri, Nicoletta; Biava, Mariangela; Droghini, P.; Atzori, ELENA MARIA; Ibba, C.; Collu, G.; Sanna, G.; Delogu, I.; Loddo, R.. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - STAMPA. - 25:11(2015), pp. 2401-2404. [10.1016/j.bmcl.2015.04.006]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/783700
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