N-((1, 3-Diphenyl-1H-pyrazol-4-yl)methyl)anilines: A novel class of anti-RSV agents. Issue 11 (1st June 2015)

• Record Type: Journal Article
• Authors: Fioravanti, Rossella; Desideri, Nicoletta; Biava, Mariangela; Droghini, Paolo; Atzori, Elena Maria; Ibba, Cristina; Collu, Gabriella; Sanna, Giuseppina; Delogu, Ilenia; Loddo, Roberta
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 11(2015)
• Page Start: 2401
• Page End: 2404
• Publication Date: 2015-06-01
• Subjects: QPZNPZUACIKDGE-UHFFFAOYSA-N; Pyrazole derivatives -- Aniline derivatives -- Antiviral activity -- Anti-RSV activity -- RNA and DNA viruses; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.04.006
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A series of N -((1, 3-diphenyl-1 H -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 (EC50 s 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.