DSpace
 

Researchspace >
General science, engineering & technology >
General science, engineering & technology >
General science, engineering & technology >

Please use this identifier to cite or link to this item: http://hdl.handle.net/10204/5233

Title: Imidazo[1,2-a]pyridin-3-amines as potential HIV-1 non-nucleoside reverse transcriptase inhibitors
Authors: Bode, ML
Gravestock, D
Moleele, SS
Van der Westhuyzen, CW
Pelly, SC
Steenkamp, PA
Hoppe, HC
Khan, T
Nkabinde, LA
Keywords: Non nucleoside reverse transcriptase inhibitor
NNRTI
HIV-1 reverse transcriptase
Imidazo[1,2-a]pyridin-3-amines
Anti-HIV MAGI assay
Groebke reaction
Antiretroviral
Imidazo[1,2-a]pyridine
Bioorganic
Medicinal chemistry
Issue Date: Jun-2011
Publisher: Elsevier
Citation: Bode, ML, Gravestock, D, Moleele, SS et al. 2011. Imidazo[1,2-a]pyridin-3-amines as potential HIV-1 non-nucleoside reverse transcriptase inhibitors. Bioorganic and Medicinal Chemistry, Vol 19(4), pp 4227-4237
Series/Report no.: Workflow request;4201
Abstract: During random screening of a small in-house library of compounds, certain substituted imidazo[1,2-a]pyridines were found to be weak allosteric inhibitors of HIV-1 reverse transcriptase (RT). A library of these compounds was prepared using the Groebke reaction and a subset of compounds prepared from 2-chlorobenzaldehyde, cyclohexyl isocyanide and a 6-substituted 2-aminopyridine showed good inhibitory activity in enzymatic (RT) and HIV anti-infectivity MAGI whole cell assays. The compound showing the best anti-HIV-1 IIIB whole cell activity (MAGI IC50 = 0.18 µM, IC90 = 1.06 µM), along with a good selectivity index (>800), was 2-(2-chlorophenyl)-3-(cyclohexylamino)imidazo[1,2-a]pyridine-5-carbonitrile 38.
Description: Copyright: 2011 Elsevier. This is the pre print version of the paper. The definitive version is published in Bioorganic and Medicinal Chemistry, Vol 19(4), pp 4227-4237
URI: http://www.sciencedirect.com/science/article/pii/S0968089611004263
http://hdl.handle.net/10204/5233
ISSN: 0968-0896
Appears in Collections:General science, engineering & technology
Discovery chemistry

Files in This Item:

File Description SizeFormat
Bode_2011.pdf455.91 kBAdobe PDFView/Open
View Statistics

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

 

Valid XHTML 1.0! DSpace Software Copyright © 2002-2010  Duraspace - Feedback