Novel Nucleoside Analogues as Effective Antiviral Agents for Zika Virus Infections.

Previously considered a neglected , Zika virus has recently emerged as a public health concern due to its ability to spread rapidly and cause severe neurological disorders, such as microcephaly in newborn babies from infected mothers, and Guillain-Barré syndrome in adults. Despite extensive efforts towards the identification of effective therapies, specific antivirals are still not available. As part of ongoing medicinal chemistry studies to identify new antiviral agents, we screened against Zika virus replication in vitro in a targeted internal library of small-molecule agents, comprising both nucleoside and non-nucleoside agents.

Microwave-assisted organic synthesis of nucleoside ProTide analogues.

A microwave enhanced synthesis of prodrug nucleotide (ProTide) analogues is presented. Comparison of conventional thermal heating reaction with microwave irradiation exemplifies the potential of the novel methodology herein presented for the selective 5'-phosphoramidate synthesis, without protection of the 3' position in the ribonucleoside.