tetano
Editor, Senior Moderator
Bioorg Med Chem. 2012 May 17. [Epub ahead of print]
Pyrrolidinobenzoic acid inhibitors of influenza virus neuraminidase: The hydrophobic side chain influences type A subtype selectivity.
Li Y, Silamkoti A, Kolavi G, Mou L, Gulati S, Air GM, Brouillette WJ.
Source
Department of Chemistry, University of Alabama at Birmingham, Birmingham, AL 35294, USA.
Abstract
Neuraminidase (NA) plays a critical role in the life cycle of influenza virus and is a target for new therapeutic agents. A series of influenza neuraminidase inhibitors with the pyrrolidinobenzoic acid scaffold containing lipophilic side chains at the C3 position have been synthesized and evaluated for influenza neuraminidase inhibitory activity. The size and geometry of the C3 side chains have been modified in order to investigate structure-activity relationships. The results indicated that size and geometry of the C3-side chain are important for selectivity of inhibition against N1 versus N2 NA, important type A influenza variants that infect man, including the highly lethal avian influenza.
Copyright ? 2012 Elsevier Ltd. All rights reserved.
PMID:
22677529
[PubMed - as supplied by publisher]
http://www.ncbi.nlm.nih.gov/pubmed/22677529
Pyrrolidinobenzoic acid inhibitors of influenza virus neuraminidase: The hydrophobic side chain influences type A subtype selectivity.
Li Y, Silamkoti A, Kolavi G, Mou L, Gulati S, Air GM, Brouillette WJ.
Source
Department of Chemistry, University of Alabama at Birmingham, Birmingham, AL 35294, USA.
Abstract
Neuraminidase (NA) plays a critical role in the life cycle of influenza virus and is a target for new therapeutic agents. A series of influenza neuraminidase inhibitors with the pyrrolidinobenzoic acid scaffold containing lipophilic side chains at the C3 position have been synthesized and evaluated for influenza neuraminidase inhibitory activity. The size and geometry of the C3 side chains have been modified in order to investigate structure-activity relationships. The results indicated that size and geometry of the C3-side chain are important for selectivity of inhibition against N1 versus N2 NA, important type A influenza variants that infect man, including the highly lethal avian influenza.
Copyright ? 2012 Elsevier Ltd. All rights reserved.
PMID:
22677529
[PubMed - as supplied by publisher]
http://www.ncbi.nlm.nih.gov/pubmed/22677529