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

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

  • Bioorg Med Chem Lett. 2015 Jun 1;25(11):2401-4. doi: 10.1016/j.bmcl.2015.04.006.
Rossella Fioravanti 1,  Nicoletta Desideri 2,  Mariangela Biava 2,  Paolo Droghini 2,  Elena Maria Atzori 2,  Cristina Ibba 3,  Gabriella Collu 3,  Giuseppina Sanna 3,  Ilenia Delogu 3,  Roberta Loddo 4
Affiliations

Affiliations

  • 1 Dipartimento di Chimica e Tecnologie del Farmaco, Università 'La Sapienza', P.le Aldo Moro, 5, 00185 Rome, Italy. Electronic address: rossella.fioravanti@uniroma1.it.
  • 2 Dipartimento di Chimica e Tecnologie del Farmaco, Università 'La Sapienza', P.le Aldo Moro, 5, 00185 Rome, Italy.
  • 3 Dipartimento di Scienze Biomediche, Università di Cagliari, 09042 Monserrato, Cagliari, Italy.
  • 4 Dipartimento di Scienze Biomediche, Università di Cagliari, 09042 Monserrato, Cagliari, Italy. Electronic address: rloddo@unica.it.
PMID: 25913116 DOI: 10.1016/j.bmcl.2015.04.006
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.

Keywords

Aniline derivatives; Anti-RSV activity; Antiviral activity; Pyrazole derivatives; RNA and DNA viruses.

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