Oseltamivir analogs with potent anti-influenza virus activity

Sumit Kumar, Steven Goicoechea, Sonu Kumar, Catherine M. Pearce, Ravi Durvasula, Prakasha Kempaiah, Brijesh Rathi, Poonam

Research output: Contribution to journalReview articlepeer-review

Abstract

Influenza A and B viruses cause seasonal worldwide influenza epidemics each winter, and are a major public health concern and cause of morbidity and mortality. A substantial reduction in influenza-related deaths can be attributed to both vaccination and administration of oseltamivir (OS), which is approved for oral administration and inhibits viral neuraminidase (NA), a transmembrane protein. OS carboxylate (OSC), the active form of OS, is formed by the action of endogenous esterase, which targets NA and is shown to significantly reduce influenza-related deaths. However, the development of resistance in various viral variants, including H3N2 and H5N1, has raised concern about the effectiveness of OS. This comprehensive review covers a range of OS analogs shown to be effective against influenza virus, comparing different types of substituent group that contribute to the activity and bioavailability of these compounds. Oseltamivir, a single effective oral drug available for the treatment of influenza infections, makes the discovery of its analogs valuable and interesting.

Original languageEnglish (US)
Pages (from-to)1389-1402
Number of pages14
JournalDrug Discovery Today
Volume25
Issue number8
DOIs
StatePublished - Aug 2020

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

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