1844-70-8Relevant academic research and scientific papers
2-Phenylimidazo[1,2-b]pyridazine derivatives highly active against Haemonchus contortus
Ali, Abdelselam,Cablewski, Teresa,Francis, Craig L.,Ganguly, Ashit K.,Sargent, Roger M.,Sawutz, David G.,Winzenberg, Kevin N.
supporting information; experimental part, p. 4160 - 4163 (2011/08/10)
A series of 2-phenylimidazo[1,2-b]pyridazine derivatives were synthesized and evaluated for their in vitro anthelmintic activity against Haemonchus contortus. The most active compounds had in vitro LD99 values of 30 nM, which is comparable to that of the benchmark commercial nematocide, Ivermectin.
Syntheses, pharmacological evaluation and molecular modelling of substituted 6-alkoxyimidazopyridazines as new ligands for the benzodiazepine receptor
Harrison, P. W.,Barlin, G. B.,Davies, L. P.,Ireland, S. J.,Matyus, P.,Wong, M. G.
, p. 651 - 662 (2007/10/03)
A series of 2,3-disubstituted-6-alkoxyimidazopyridazines has been synthesized and evaluated for in vitro affinity for the benzodiazepine receptor (BZR). 3-(Benzamidomethyl or substituted benzamidomethyl)-6-methoxy-2-(3,4-methylenedioxyphenyl)imidazopyridazines were found to be the most potent BZR ligands (eg, 4a, IC50 7 nM; 4e, IC50 14 nM; 4v, IC50 8 nM).Imidazopyridazines unsubstituted in the 3-position, or containing bulkier alkoxy groups in the 6-position, were found to bind less strongly to the BZR.Selected compounds from the series wereidentified from in vitro GABA-shift experiments as BZR agonists.Molecular modelling has been employed to identify the common pharmacophoric points of lipophilic and hydrogen bonding, ligand-receptor interaction and areas of steric hindrance for these substituted imidazopyridazines at the BZR. - Keywords: imidazopyridazine; benzodiazepine receptor; structure-activity relationship; molecullar modelling
