Highly potent and long-acting trimeric and tetrameric inhibitors of influenza virus neuraminidase.
A set of trimeric and tetrameric derivatives 6-11 of the influenza virus neuraminidase inhibitor zanamivir 1 have been synthesized by coupling a common monomeric zanamivir derivative 3 onto various multimeric carboxylic acid core groups. These discrete multimeric compounds are all significantly more antiviral than zanamivir and also show outstanding long-lasting protective activity when tested in mouse influenza infectivity experiments.
Biota Chemistry Laboratory, School of Chemistry, Monash University, PO Box 23, Victoria 3800, Australia. kwatson@edu.au
Keith G
KG
Watson
Rachel
R
Cameron
Rob J
RJ
Fenton
David
D
Gower
Stephanie
S
Hamilton
Betty
B
Jin
Guy Y
GY
Krippner
Angela
A
Luttick
Darryl
D
McConnell
Simon J F
SJ
MacDonald
Andy M
AM
Mason
Van
V
Nguyen
Simon P
SP
Tucker
Wen-Yang
WY
Wu
D000818:Animals; D000998:Antiviral Agents / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D006146:Guanidines; D009980:Influenza A virus / Q000187:drug effects / Q000201:enzymology*; D051379:Mice; D009439:Neuraminidase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D009976:Orthomyxoviridae Infections / Q000188:drug therapy / Q000201:enzymology; D011714:Pyrans; D012794:Sialic Acids / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D053243:Zanamivir
D000998:Antiviral Agents; D004791:Enzyme Inhibitors; D006146:Guanidines; D011714:Pyrans; D012794:Sialic Acids; D009439:Neuraminidase; D053243:Zanamivir