Title: Identification and synthesis of 1,4-disubstituted piperidines as new entry inhibitors of H1N1 influenza virus
Authors: Velazquez, Sonsoles
de Castro, Sonia
Vanderlinden, Evelien
Naesens, Lieve
Camarasa, María José
Issue Date: May-2015
Host Document: Abstract book pages:104
Conference: 28th International Conference on Antiviral Research location:Rome, Italy date:11-15 May 2015
Article number: 104
Abstract: The recent outbreaks of the highly pathogenic avian A/H5N1 and pandemic A/H1N1/2009 influenza viruses have emphasized the
need for anti-influenza drug discovery. The piperidine nucleus is an attractive drug template exploited in agents with applications
as anti-histaminic, anti-inflammatory, fungicidal, bactericidal, anticancer, analgesic, CNS stimulant and or anti-depressant activities.
In an effort to discover novel compounds as potential anti-influenza drugs, several molecules of our diverse in-house library
were screened for anti-influenza virus activity. Following this approach, we identified disubstituted piperidine-based compounds
as interesting hit compounds that display low micromolar activity against the influenza A/PR/8/34 virus (A/H1N1) in cell culture.
To investigate the structure-activity relationships, several analogues were easily synthesized by a one-step Ugi four-component
reaction from an amine, an isocyanide, N-substituted piperidones and carboxylic acid components. Time-of-addition studies
showed that the compounds act during influenza virus entry. Mechanistic studies are ongoing to precisely identify their antiviral
target, and explain the basis for the observed H1N1 specificity.
Publication status: published
KU Leuven publication type: IMa
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)

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