TY - JOUR
T1 - Oseltamivir analogs with potent anti-influenza virus activity
AU - Kumar, Sumit
AU - Goicoechea, Steven
AU - Kumar, Sonu
AU - Pearce, Catherine M.
AU - Durvasula, Ravi
AU - Kempaiah, Prakasha
AU - Rathi, Brijesh
AU - Poonam,
N1 - Publisher Copyright:
© 2020 Elsevier Ltd
PY - 2020/8
Y1 - 2020/8
N2 - 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.
AB - 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.
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U2 - 10.1016/j.drudis.2020.06.004
DO - 10.1016/j.drudis.2020.06.004
M3 - Review article
C2 - 32554062
AN - SCOPUS:85086716125
SN - 1359-6446
VL - 25
SP - 1389
EP - 1402
JO - Drug Discovery Today
JF - Drug Discovery Today
IS - 8
ER -