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Oseltamivir hydroxamate and acyl sulfonamide derivatives as influenza neuraminidase inhibitors

tetano

tetano

Editor, Senior Moderator
Bioorg Med Chem. 2014 Oct 25;22(23):6647-6654. doi: 10.1016/j.bmc.2014.10.005. [Epub ahead of print]
Oseltamivir hydroxamate and acyl sulfonamide derivatives as influenza neuraminidase inhibitors.
Hong BT1, Chen CL1, Fang JM2, Tsai KC3, Wang SY4, Huang WI4, Cheng YS4, Wong CH4.
Author information
Abstract

Tamiflu, the ethyl ester form of oseltamivir carboxylic acid (OC), is the first orally available anti-influenza drug for the front-line therapeutic option. In this study, the OC-hydroxamates, OC-sulfonamides and their guanidino congeners (GOC) were synthesized. Among them, an OC-hydroxamate 7d bearing an O-(2-indolyl)propyl substituent showed potent NA inhibition (IC50=6.4nM) and good anti-influenza activity (EC50=60.1nM) against the wild-type H1N1 virus. Two GOC-hydroxamates (9b and 9d) and one GOC-sulfonamide (12a) were active to the tamiflu-resistant H275Y virus (EC50=2.3-6.9μM).

Copyright ? 2014 Elsevier Ltd. All rights reserved.
KEYWORDS:

Acyl sulfonamide; Bioisosteres; Hydroxamate; Influenza; Neuraminidase inhibitor; Oseltamivir

PMID:
25456388
[PubMed - as supplied by publisher]

http://www.ncbi.nlm.nih.gov/pubmed/25456388
 
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