Bode, MLGravestock, DMoleele, SSVan der Westhuyzen, Christiaan WPelly, SCSteenkamp, PAHoppe, HCKhan, TNkabinde, LA2011-10-132011-10-132011-06Bode, 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 4227-42370968-0896http://www.sciencedirect.com/science/article/pii/S0968089611004263http://hdl.handle.net/10204/5233Copyright: 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 4227-4237During 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.enNon nucleoside reverse transcriptase inhibitorNNRTIHIV-1 reverse transcriptaseImidazo[1,2-a]pyridin-3-aminesAnti-HIV MAGI assayGroebke reactionAntiretroviralImidazo[1,2-a]pyridineBioorganicMedicinal chemistryArticleBode, 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/10204/5233Bode, 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/10204/5233Bode 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.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 -