- 2-Phenylimidazo[1,2-b]pyridazine derivatives highly active against Haemonchus contortus
-
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.
- Ali, Abdelselam,Cablewski, Teresa,Francis, Craig L.,Ganguly, Ashit K.,Sargent, Roger M.,Sawutz, David G.,Winzenberg, Kevin N.
-
scheme or table
p. 4160 - 4163
(2011/08/10)
-
- CONTROL OF PARASITES IN ANIMALS BY THE USE OF IMIDAZO[1,2-B]PYRIDAZINE DERIVATIVES
-
Novel imidazo[1,2-b]pyridazine compounds useful for controlling parasites in animals and methods of treatment of parasite infestation in animals using the compounds are disclosed. Formula (I).
- -
-
Page/Page column 21
(2008/06/13)
-
- A revision of the alcoholysis and alkanethiolysis of 3-amino-6-chloropyridazine
-
The synthesis of 3-amino-6-alkoxy- and 3-amino-6-alkylthiopyridazines via nucleophilic aromatic substitution on 3-amino-6-chloropyridazine is described. In contrast to literature reports, no pressure tube is required to perform these reactions.
- Maes,Lemiere,Dommisse,Haemers
-
p. 1215 - 1218
(2007/10/03)
-
- Syntheses, pharmacological evaluation and molecular modelling of substituted 6-alkoxyimidazopyridazines as new ligands for the benzodiazepine receptor
-
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
- Harrison, P. W.,Barlin, G. B.,Davies, L. P.,Ireland, S. J.,Matyus, P.,Wong, M. G.
-
p. 651 - 662
(2007/10/03)
-