Literature DB >> 25913116

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

Rossella Fioravanti1, Nicoletta Desideri2, Mariangela Biava2, Paolo Droghini2, Elena Maria Atzori2, Cristina Ibba3, Gabriella Collu3, Giuseppina Sanna3, Ilenia Delogu3, Roberta Loddo4.   

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.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

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

Mesh:

Substances:

Year:  2015        PMID: 25913116     DOI: 10.1016/j.bmcl.2015.04.006

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

Review 1.  Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review.

Authors:  Khalid Karrouchi; Smaail Radi; Youssef Ramli; Jamal Taoufik; Yahia N Mabkhot; Faiz A Al-Aizari; M'hammed Ansar
Journal:  Molecules       Date:  2018-01-12       Impact factor: 4.411

2.  Unveiling the Different Chemical Reactivity of Diphenyl Nitrilimine and Phenyl Nitrile Oxide in [3+2] Cycloaddition Reactions with (R)-Carvone through the Molecular Electron Density Theory.

Authors:  Mar Ríos-Gutiérrez; Luis R Domingo; M'hamed Esseffar; Ali Oubella; My Youssef Ait Itto
Journal:  Molecules       Date:  2020-02-28       Impact factor: 4.411

  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.