1218933-95-9Relevant academic research and scientific papers
Imidazo[1,2-a]pyridin-3-amines as potential HIV-1 non-nucleoside reverse transcriptase inhibitors
Bode, Moira L.,Gravestock, David,Moleele, Simon S.,Van Der Westhuyzen, Christiaan W.,Pelly, Stephen C.,Steenkamp, Paul A.,Hoppe, Heinrich C.,Khan, Tasmiyah,Nkabinde, Lindiwe A.
experimental part, p. 4227 - 4237 (2011/08/21)
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.
IMIDAZOPYRIDINES AND IMIDAZOPYRIMIDINES AS HIV-I REVERSE TRANSCRIPTASE INHIBITORS
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Page/Page column 15, (2010/04/25)
The invention provides compounds of formula A or B which are useful in the treatment of a subject infected with HIV.
