tetano
Editor, Senior Moderator
J Med Chem. 2014 Mar 20. [Epub ahead of print]
Oseltamivir analogues bearing N-substituted guanidines as potent neuraminidase inhibitors.
Mooney CA, Johnson SA, 't Hart P, Quarles van Ufford L, de Haan CA, Moret EE, Martin NI.
Abstract
A series of oseltamivir analogues bearing an N-substituted guanidine unit were prepared and evaluated as inhibitors of neuraminidases from four strains of influenza. The two most potent analogues identified contain relatively small N-guanidine substituents (N-methyl and N-hydroxyl) and display enhanced inhibition with IC50 values in the low nM range against neuraminidases from both wild-type and oseltamivir-resistant strains. Potential advantages of including the N-hydroxyguanidine moiety in neuraminidase inhibitors are also discussed.
PMID:
24649802
[PubMed - as supplied by publisher]
http://www.ncbi.nlm.nih.gov/pubmed/24649802
Oseltamivir analogues bearing N-substituted guanidines as potent neuraminidase inhibitors.
Mooney CA, Johnson SA, 't Hart P, Quarles van Ufford L, de Haan CA, Moret EE, Martin NI.
Abstract
A series of oseltamivir analogues bearing an N-substituted guanidine unit were prepared and evaluated as inhibitors of neuraminidases from four strains of influenza. The two most potent analogues identified contain relatively small N-guanidine substituents (N-methyl and N-hydroxyl) and display enhanced inhibition with IC50 values in the low nM range against neuraminidases from both wild-type and oseltamivir-resistant strains. Potential advantages of including the N-hydroxyguanidine moiety in neuraminidase inhibitors are also discussed.
PMID:
24649802
[PubMed - as supplied by publisher]
http://www.ncbi.nlm.nih.gov/pubmed/24649802