The Influenza A virus is currently able to evade chemotherapeutic measures due to increased resistance to antivirals.  This makes it pertinent to develop more potent drug candidates in order to prevent future pandemic.  Here, a new set of antiviral candidates are designed and synthesized to produce sulfur analogues of the current antiviral Amantadine�.  The rationale behind this approach is to form a larger base on the molecules, allowing better obstruction of the mutated protein channel, which is the target of these adamantane drugs.  The mechanism of action of the ion channel blockers has recently been elucidated, yet questions remain in the development of drug resistance.  We report the multi-step syntheses and characterization of potential antiviral compounds as ion channel blockers. The drug activity is studied by monitoring the host-guest interactions as a model of drug action via 2D NOESY NMR spectroscopy and tandem mass spectrometry prior to in vitro testing.

Synthesis and characterization of new influenza A M2 ion channel blockers

244th National Meeting (2012)

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