Literature DB >> 11278042

Synthesis and influenza virus sialidase inhibitory activity of analogues of 4-Guanidino-Neu5Ac2en (Zanamivir) modified in the glycerol side-chain.

D M Andrews1, P C Cherry, D C Humber, P S Jones, S P Keeling, P F Martin, C D Shaw, S Swanson.   

Abstract

Analogues of 4-Guanidino-Neu5Ac2en (Zanamivir) have been prepared containing carbamate substituents at the 7-hydroxy position. (4S,5R,6R)-5-Acetylamino-6-[1R-[(6-aminohexyl)carbamoyloxy]-2R,3-dihydroxypropyl]-4-guanidino-5,6-dihydro-4H-pyran-2carboxylic acid and (4S,5R,6R)-5-Acetylamino-6-[1R-[heptylcarbamoyloxy]-2R,3-dihydroxypropyl]-4-guanidino-5,6-dihydro4H-pyran2-carboxylic acid were the two analogues possessing activity comparable to Zanamivir, showing potent inhibition of influenza virus sialidases and good antiviral activity in vitro.

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Year:  1999        PMID： 11278042     DOI： 10.1016/s0223-5234(00)80026-4

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN： 0223-5234            Impact factor:   6.514


  5 in total

1.  Potent and long-acting dimeric inhibitors of influenza virus neuraminidase are effective at a once-weekly dosing regimen.

Authors:  Simon J F Macdonald; Keith G Watson; Rachel Cameron; David K Chalmers; Derek A Demaine; Rob J Fenton; David Gower; J Nicole Hamblin; Stephanie Hamilton; Graham J Hart; Graham G A Inglis; Betty Jin; Haydn T Jones; Darryl B McConnell; Andy M Mason; Van Nguyen; Ian J Owens; Nigel Parry; Phillip A Reece; Stephen E Shanahan; Donna Smith; Wen-Yang Wu; Simon P Tucker
Journal:  Antimicrob Agents Chemother       Date:  2004-12       Impact factor: 5.191

2.  Bifunctional polymeric inhibitors of human influenza A viruses.

Authors:  Jayanta Haldar; Luis Alvarez de Cienfuegos; Terrence M Tumpey; Larisa V Gubareva; Jianzhu Chen; Alexander M Klibanov
Journal:  Pharm Res       Date:  2009-12-15       Impact factor: 4.200

3.  Attaching zanamivir to a polymer markedly enhances its activity against drug-resistant strains of influenza a virus.

Authors:  Alisha K Weight; Jayanta Haldar; Luis Alvarez de Cienfuegos; Larisa V Gubareva; Terrence M Tumpey; Jianzhu Chen; Alexander M Klibanov
Journal:  J Pharm Sci       Date:  2010-08-25       Impact factor: 3.534

4.  Zanamivir conjugated to poly-L-glutamine is much more active against influenza viruses in mice and ferrets than the drug itself.

Authors:  Alisha K Weight; Jessica A Belser; Terrence M Tumpey; Jianzhu Chen; Alexander M Klibanov
Journal:  Pharm Res       Date:  2013-09-25       Impact factor: 4.200

Review 5.  Development of effective anti-influenza drugs: congeners and conjugates - a review.

Authors:  Jiun-Jie Shie; Jim-Min Fang
Journal:  J Biomed Sci       Date:  2019-10-23       Impact factor: 8.410
  5 in total

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