365213-55-4Relevant academic research and scientific papers
Design, Synthesis, and Biological Evaluation of Novel Fluorescent Probes Targeting the 18-kDa Translocator Protein
Wongso, Hendris,Yamasaki, Tomoteru,Kumata, Katsushi,Ono, Maiko,Higuchi, Makoto,Zhang, Ming-Rong,Fulham, Michael J.,Katsifis, Andrew,Keller, Paul A.
, p. 1902 - 1916 (2021)
A series of fluorescent probes from the 6-chloro-2-phenylimidazo[1,2-a]pyridine-3-yl acetamides ligands featuring the 7-nitro-2-oxa-1,3-diazol-4-yl (NBD) moiety has been synthesized and biologically evaluated for their fluorescence properties and for thei
Synthesis and biological evaluation of substituted [18F] imidazo[1,2-a]pyridines and [18F]pyrazolo[1,5-a]pyrimidines for the study of the peripheral benzodiazepine receptor using positron emission tomography
Fookes, Christopher J. R.,Pham, Tien Q.,Mattner, Filomena,Greguric, Ivan,Loc'h, Christian,Liu, Xiang,Berghofer, Paula,Shepherd, Rachael,Gregoire, Marie-Claude,Katsifis, Andrew
experimental part, p. 3700 - 3712 (2009/04/11)
The fluoroethoxy and fluoropropoxy substituted 2-(6-chloro-2-phenyl) imidazo[1,2-a]pyridin-3-yl)-N,N-diethylacetamides 8 (PBR102) and 12 (PBR111) and 2-phenyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)-N,N-diethylacetamides 15 (PBR099) and 18 (PBR146) wer
A structure-activity relationship study of the affinity of selected imidazo[1,2-a]pyridine derivatives, congeners of zolpidem, for the ω1-subtype of the benzodiazepine receptor
Lange,Karolak-Wojciechowska,Wejroch,Rump
, p. 43 - 52 (2007/10/03)
A series of 6-substituted 2-aryl-N,N-dimethylimidazol [1,2-a]pyridine-3-acetamides, congeners of zolpidem and alpidem, was synthesized and tested in vitro for binding with the benzodiazepine receptor in the competition with 3H-zolpidem as an ω1-selective radioligand. Molecular electrostatic potential (MEP) and the HOMO and LUMO energies were calculated for the compounds by semi-empirical quantum chemistry methods. The lipophilicity parameter of the compounds, expressed as the logarithm of the octanol-water partition coefficient (log P), was calculated; alternatively, standard values of the Hansch hydrophobic substituent constants π were used. In agreement with earlier investigations on the benzodiazepine receptor ligands with a high preference for the ω1-subtype, a quantitative correlation of the biological data with molecular parameters has revealed a significant dependence (r=0.954) of the binding affinity (IC50) on the deepest MEP minimum, in this case associated with the amide carbonyl oxygen atom. The lipophilicity parameters were found to be of lower significance.
