1152034-94-0Relevant articles and documents
Identification of a 3-aminoimidazo[1,2-a]pyridine inhibitor of HIV-1 reverse transcriptase
Elleder, Daniel,Baiga, Thomas J.,Russell, Rebecca L.,Naughton, John A.,Hughes, Stephen H.,Noel, Joseph P.,Young, John A.T.
, (2012)
Background: Despite the effectiveness of highly active antiretroviral therapy (HAART), there remains an urgent need to develop new human immunodeficiency virus type 1 (HIV-1) inhibitors with better pharmacokinetic properties that are well tolerated, and t
Diverse Oxidative C(sp2)-N Bond Cleavages of Aromatic Fused Imidazoles for Synthesis of α-Ketoamides and N-(pyridin-2-yl)arylamides
Xu, Fangzhou,Wang, Yanyan,Xun, Xiwei,Huang, Yun,Jin, Zhichao,Song, Baoan,Wu, Jian
, p. 8411 - 8422 (2019/05/17)
An efficient and chemoselective C(sp2)-N bond cleavage of aromatic imidazo[1,2-a]pyridine molecules is developed. A broad scope of amide compounds such as α-ketoamides and N-(pyridin-2-yl)arylamides are afforded as the final products in up to quantitative yields. Diverse C-N bond cleavages are controlled by the oxidative species used in this transformation, with various amide products afforded in a chemoselective fashion. A preliminary study indicated that some α-ketoamides exhibit anti-Tobacco Mosaic Virus activity for potential use in plant protection.
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.