ResearchSpace

Imidazo[1,2-a]pyridin-3-amines as potential HIV-1 non-nucleoside reverse transcriptase inhibitors

Show simple item record

dc.contributor.author Bode, ML
dc.contributor.author Gravestock, D
dc.contributor.author Moleele, SS
dc.contributor.author Van der Westhuyzen, Christiaan W
dc.contributor.author Pelly, SC
dc.contributor.author Steenkamp, PA
dc.contributor.author Hoppe, HC
dc.contributor.author Khan, T
dc.contributor.author Nkabinde, LA
dc.date.accessioned 2011-10-13T10:18:06Z
dc.date.available 2011-10-13T10:18:06Z
dc.date.issued 2011-06
dc.identifier.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 en_US
dc.identifier.issn 0968-0896
dc.identifier.uri http://www.sciencedirect.com/science/article/pii/S0968089611004263
dc.identifier.uri http://hdl.handle.net/10204/5233
dc.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 en_US
dc.description.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. en_US
dc.language.iso en en_US
dc.publisher Elsevier en_US
dc.relation.ispartofseries Workflow request;4201
dc.subject Non nucleoside reverse transcriptase inhibitor en_US
dc.subject NNRTI en_US
dc.subject HIV-1 reverse transcriptase en_US
dc.subject Imidazo[1,2-a]pyridin-3-amines en_US
dc.subject Anti-HIV MAGI assay en_US
dc.subject Groebke reaction en_US
dc.subject Antiretroviral en_US
dc.subject Imidazo[1,2-a]pyridine en_US
dc.subject Bioorganic en_US
dc.subject Medicinal chemistry en_US
dc.title Imidazo[1,2-a]pyridin-3-amines as potential HIV-1 non-nucleoside reverse transcriptase inhibitors en_US
dc.type Article en_US
dc.identifier.apacitation Bode, M., Gravestock, D., Moleele, S., Van der Westhuyzen, C. W., Pelly, S., Steenkamp, P., ... Nkabinde, L. (2011). Imidazo[1,2-a]pyridin-3-amines as potential HIV-1 non-nucleoside reverse transcriptase inhibitors. http://hdl.handle.net/10204/5233 en_ZA
dc.identifier.chicagocitation Bode, ML, D Gravestock, SS Moleele, Christiaan W Van der Westhuyzen, SC Pelly, PA Steenkamp, HC Hoppe, T Khan, and LA Nkabinde "Imidazo[1,2-a]pyridin-3-amines as potential HIV-1 non-nucleoside reverse transcriptase inhibitors." (2011) http://hdl.handle.net/10204/5233 en_ZA
dc.identifier.vancouvercitation Bode M, Gravestock D, Moleele S, Van der Westhuyzen CW, Pelly S, Steenkamp P, et al. Imidazo[1,2-a]pyridin-3-amines as potential HIV-1 non-nucleoside reverse transcriptase inhibitors. 2011; http://hdl.handle.net/10204/5233. en_ZA
dc.identifier.ris TY - Article AU - Bode, ML AU - Gravestock, D AU - Moleele, SS AU - Van der Westhuyzen, Christiaan W AU - Pelly, SC AU - Steenkamp, PA AU - Hoppe, HC AU - Khan, T AU - Nkabinde, LA AB - 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. DA - 2011-06 DB - ResearchSpace DP - CSIR KW - Non nucleoside reverse transcriptase inhibitor KW - NNRTI KW - HIV-1 reverse transcriptase KW - Imidazo[1,2-a]pyridin-3-amines KW - Anti-HIV MAGI assay KW - Groebke reaction KW - Antiretroviral KW - Imidazo[1,2-a]pyridine KW - Bioorganic KW - Medicinal chemistry LK - https://researchspace.csir.co.za PY - 2011 SM - 0968-0896 T1 - Imidazo[1,2-a]pyridin-3-amines as potential HIV-1 non-nucleoside reverse transcriptase inhibitors TI - Imidazo[1,2-a]pyridin-3-amines as potential HIV-1 non-nucleoside reverse transcriptase inhibitors UR - http://hdl.handle.net/10204/5233 ER - en_ZA


Files in this item

Thumbnail
Name: Bode_2011.pdf
Size: 455.9Kb
Format: PDF
View/Open

This item appears in the following Collection(s)

Show simple item record