Journal of Medicinal Chemistry · 2010 · 45 citations · 21 references
PharmacyMedicinal ChemistryPharmacologyDrug DesignDrug DiscoveryVirologyAntiviral PharmacologyChemical Library DesignEnzyme InhibitionScaffold HoppingAntiviral Drug DesignAntiviral Structure-activity RelationshipsChemical Scaffold HoppingInfluenza Antiviral ResistanceScaffold-based Library Design
Although amantadine derivatives are the only M2 drugs for influenza virus A, their use is limited in the U.S. because of drug resistance. Here we report the identification of multiple M2 inhibitors that were rapidly generated through focused screening of a small primary amine library that was designed using a scaffold-hopping strategy based on amantadine. These compounds are as active as amantadine and might be hits for further lead generation processes.
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Structure and mechanism of the M2 proton channel of influenza A virus
Jason R. Schnell, James J. Chou · Nature · 2008 · 1.1K citations
Life Sciences, Biology, Biophysics +12
Structural basis for the function and inhibition of an influenza virus proton channel
Amanda L. Stouffer, Rudresh Acharya, David Salom et al. · Nature · 2008 · 640 citations · Full text
Life Sciences, Biology, Biophysics +14