tetano
Editor, Senior Moderator
Drug Discov Today
. 2020 Jun 15;S1359-6446(20)30229-4.
doi: 10.1016/j.drudis.2020.06.004. Online ahead of print.
Oseltamivir Analogs With Potent Anti-Influenza Virus Activity
Sumit Kumar[SUP] 1 [/SUP], Steven Goicoechea[SUP] 2 [/SUP], Sonu Kumar[SUP] 3 [/SUP], Catherine M Pearce[SUP] 4 [/SUP], Ravi Durvasula[SUP] 5 [/SUP], Prakasha Kempaiah[SUP] 5 [/SUP], Brijesh Rathi[SUP] 6 [/SUP], Poonam[SUP] 7 [/SUP]
Affiliations
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.
. 2020 Jun 15;S1359-6446(20)30229-4.
doi: 10.1016/j.drudis.2020.06.004. Online ahead of print.
Oseltamivir Analogs With Potent Anti-Influenza Virus Activity
Sumit Kumar[SUP] 1 [/SUP], Steven Goicoechea[SUP] 2 [/SUP], Sonu Kumar[SUP] 3 [/SUP], Catherine M Pearce[SUP] 4 [/SUP], Ravi Durvasula[SUP] 5 [/SUP], Prakasha Kempaiah[SUP] 5 [/SUP], Brijesh Rathi[SUP] 6 [/SUP], Poonam[SUP] 7 [/SUP]
Affiliations
- PMID: 32554062
- DOI: 10.1016/j.drudis.2020.06.004
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.