Synthesis and quantitative structure-activity relationship study of substituted imidazophosphor ester based tetrazolo[1,5-b]pyridazines as antinociceptive/anti-inflammatory agents.
A high-yielding general synthesis of imidazophosphor ester based tetrazolo[1,5-b]pyridazines is described. A conjugated reaction between 3,6-diazidopyridazine and different types of phosphonyl carbanion reagents followed by intramolecular cyclization afforded the target products, by using sodium ethanolate solution as a reaction medium. Among the products, five compounds, at a dose of 50 mg per kilogram body weight, showed a notable antinociceptive and anti-inflammatory activity without toxic side-effects.
Chemical Industries Division, National Research Centre, Elbohouth St. D-12311, Dokki, Cairo, Egypt.
Wafaa M
WM
Abdou
Neven A
NA
Ganoub
Eman
E
Sabry
antinociceptive/anti-inflammatory agents; imidazophosphor esters; phosphonyl carbanions; ring closure; tetrazolo[1,5-b]pyridazine