Novel inhibitors of influenza sialidases related to zanamivir. Heterocyclic replacements of the glycerol sidechain

Bioorganic and Medicinal Chemistry Letters

Volumn 7, Issue 17, 1997, Pages 2239-2242

  Smith, Paul W ^a   Whittington, Andrew R ^a   Sollis, Steven L ^a   Howes, Peter D ^a   Taylor, Neil R ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

GLYCOSIDASE INHIBITOR; VIRUS SIALIDASE; ZANAMIVIR;

ANTIVIRAL ACTIVITY; ARTICLE; CONFORMATIONAL TRANSITION; DRUG SYNTHESIS; INFLUENZA VIRUS; NONHUMAN; STRUCTURE ACTIVITY RELATION;

EID: 0030930825     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(97)00399-5     Document Type: Article

References (11)

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3. Bischofberger, N.W.; Kim, C.U.; Lew, W.; Liu, H.; Williams, M.A. Preparation of selective inhibitors of viral or bacterial neuraminidases. PCT Int. Appl., WO 9626933. CAN 125:300503.
4. Kim, C.U.; Lew, W.; Williams, M.A.; Zhang, L.; Liu, H.; Swaminathan, S.; Bischofberger, N.; Chen, M.S.; Tai, C.Y.; Mendel, D.B.; Laver, W.G.; Stevens, R.C. J. Am. Chem. Soc. 1997, 119, 681.
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7. Doyle, K.M.; Kurzer, F. Synthesis 1974, 583.
8. 50 value quoted is the concentration of inhibitor required to reduce the enzymic activity in this preparation by 50%. Values for secondary and tertiary carboxamides 3a and 3b and zanamivir 1 are included in the table for comparison
9. Potier, M.L.; Mameli, L.; Belisle, M.; Dallaire, L.; Melancon, S.B Anal Biochem. 1979, 94, 287
10. Woods, J.M.; Bethell, R.C.; Coates, J.A.V.; Healy, N.; Hiscox, S.A.; Pearson, B.A.; Ryan, M.; Ticehurst, J.; Tilling, J.; Walcott, S.M.; Penn, C.R. Antimicrobial Agents Chemother. 1993, 37, 1473.
11. 6