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Adenine derivatives, in particular the scaffold bearing the acyclic nucleoside phosphonates(ANPS), possess signi fi cant antiviral and cytostatic activity. Till now, several effective adenine derivatives have been marketed for the treatment of HIV, HBV, CMV and other virus-infected diseases. These compounds are represented by tenofovir(PMPA), a medicine for both HIV and HBV, and adefovir as an anti-HBV agent. More than this, other analogs, such as GS9148, GS9131, and GS7340, are also wellknown anti-viral agents that have been progressed to the clinical studies for their excellent activity. In general, the structures of these compounds include an adenine nucleobase linked to a phosphonate side chain. Considerable structural modi fi cations on the scaffold itself and the peripheral sections were made.The structure-activity relationships(SARs) of this skeleton will provide valuable clues to identify more effective adenine derivatives as antiviral drugs. Here, we systematically summarized the SARs of the adenine derivatives, and gave important information for further optimizing this template.
Adenine derivatives, in particular the scaffold bearing the acyclic nucleoside phosphonates (ANPS), possess signi fi cant antiviral and cytostatic activity. Till now, several effective adenine derivatives have been marketed for the treatment of HIV, HBV, CMV and other virus-infected diseases These compounds are represented by tenofovir (PMPA), a medicine for both HIV and HBV, and adefovir as an anti-HBV agent. More than this, other analogs, such as GS9148, GS9131, and GS7340, are also well known anti-viral agents that have been progressed to the clinical studies for their excellent activity. In general, the structures of these compounds have an progressed to the clinical studies for their excellent activity. structure-activity relationships (SARs) of this skeleton will provide valuable clues to identify more effective adenine derivatives as antiviral drugs. Here, the SARs of the adenine derivatives, and gave important information for further optimizing this template.