Synthesis and vasodilatory activity of some amide derivatives of 6-(4-carboxymethyloxyphenyl)-4,5-dihydro-3(2H)-pyridazinone

Synthesis and vasodilatory activity of some amide derivatives of 6-(4-carboxymethyloxyphenyl)-4,5-dihydro-3(2H)-pyridazinone are reported. An effect of substitution at 2-position of pyridazinone ring on vasodilatory potential has also been explored. The most active compound 6-[4-(2-oxo-2-pyrrolidin-1-yl-ethoxy)phenyl]-2-(4-fluorophenyl)-4,5-dihydropyridazin-3(2H)-one (11) exhibited vasodilating activity in nanomolar range (IC50 = 0.051 μM).

Graphical abstractSynthesis and vasodilatory activity of some new amide derivatives of 6-(4-carboxymethyloxyphenyl)4,5-dihydro-3(2H)-pyridazinone are reported. The effect of 2-substitution on vasodilatory potential has also been explored.Figure optionsDownload full-size imageDownload as PowerPoint slide