Synthesis of N-4-Pyridyl Amide Derivatives of N-Diisopropyloxyphosphoryl Amino Acids and Antidotal Activity of Tetrodotoxin (TTX)

Some novel 4-aminopyridine derivatives of the title compounds containing the unit of N-diisopropyloxyphosphoryl amino acids were synthesized. Their structures were confirmed by IR, H-1 NMR, C-13 NMR, and mass spectra. In the present work, a group of 4-aminopyridine derivatives were synthesized in order to find novel structure with higher antagonize effects and lower toxity. On the other hand, their fragmentation behaviors were investigated by positive ion electrospray ionization mass spectrometry in conjunction with tandem mass spectrometry. The preliminary bioassay results showed that chemical modification of 4-aminopyridine possessed stronger bioactivity of antidote tetrodotoxin intoxication.