Research paperSynthesis and antiviral evaluation of cyclopentyl nucleoside phosphonates

Add time:08/14/2019    Source:sciencedirect.com

The synthesis of both 2ʹ-hydroxy-3ʹ-deoxy and 2ʹ-deoxy-3ʹ-hydroxy cyclopentyl nucleoside phosphonates with the natural nucleobases adenine, thymine, cytosine and guanine from a single precursor has been performed. The guanine containing analogues showed antiviral activity. Especially the 3ʹ-deoxy congener 23 was active, displaying an EC50 of 5.35 μM against TK+ VZV strain and an EC50 of 8.83 μM against TK− VZV strain, besides lacking cytotoxicity. However, the application of phosphonodiamidate prodrug strategy did not lead to a boost in antiviral activity.

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