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.
Watson
Keith G
KG
Biota Chemistry Laboratory, School of Chemistry, Monash University, PO Box 23, Victoria 3800, Australia. kwatson@edu.au
Cameron
Rachel
R
Fenton
Rob J
RJ
Gower
David
D
Hamilton
Stephanie
S
Jin
Betty
B
Krippner
Guy Y
GY
Luttick
Angela
A
McConnell
Darryl
D
MacDonald
Simon J F
SJ
Mason
Andy M
AM
Nguyen
Van
V
Tucker
Simon P
SP
Wu
Wen-Yang
WY
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