tetano
Editor, Senior Moderator
J Med Chem. 2012 Sep 27. [Epub ahead of print]
Exploring the Interactions of Unsaturated Glucuronides with Influenza Virus Sialidase.
Bhatt B, B?hm R, Kerry PS, Dyason JC, Russell RJ, Thomson RJ, von Itzstein M.
Abstract
A series of C3-O-functionalized 2-acetamido-2-deoxy-Δ4-β-D-glucuronides were synthesized to explore non-charge interactions in subsite 2 of the influenza virus sialidase active site. In complex with A/N8 sialidase the parent compound (C3 OH) inverts its solution conformation to bind with all substituents well positioned in the active site. The parent compound inhibits influenza virus sialidase at a sub-microM level; the introduction of small alkyl substituents or an acetyl group at C3 is also tolerated.
PMID:
23017008
[PubMed - as supplied by publisher]
http://www.ncbi.nlm.nih.gov/pubmed/23017008
Exploring the Interactions of Unsaturated Glucuronides with Influenza Virus Sialidase.
Bhatt B, B?hm R, Kerry PS, Dyason JC, Russell RJ, Thomson RJ, von Itzstein M.
Abstract
A series of C3-O-functionalized 2-acetamido-2-deoxy-Δ4-β-D-glucuronides were synthesized to explore non-charge interactions in subsite 2 of the influenza virus sialidase active site. In complex with A/N8 sialidase the parent compound (C3 OH) inverts its solution conformation to bind with all substituents well positioned in the active site. The parent compound inhibits influenza virus sialidase at a sub-microM level; the introduction of small alkyl substituents or an acetyl group at C3 is also tolerated.
PMID:
23017008
[PubMed - as supplied by publisher]
http://www.ncbi.nlm.nih.gov/pubmed/23017008