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Chinese Journal of Organic Chemistry >

2012 , Vol. 32 >Issue 01: 178 - 182

DOI: https://doi.org/10.6023/cjoc1105102

Notes

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

  • FANG Hua ,
  • CHEN Wei-Zhu ,
  • HONG Bi-Hong ,
  • ZHANG Yi-Ping ,
  • YI Rui-Zao
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  • The Third Institute of Oceanography of the State Oceanic Administration, Xiamen 361005

Received date: 2011-05-10

  Revised date: 2011-07-25

  Online published: 2011-09-15

Supported by

Project supported by the National Natural Science Foundation of China (No. 40806032), and the Natural Science Foundation of Fujian Province (Nos. 2009J05099, 2010NZ0001-2).

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Abstract

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, 1H NMR, 13C 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.

Key words： 4-aminopyridine (4-AP); tetrodotoxin (TTX); ESI-MS/MS; antidote

Cite this article

FANG Hua , CHEN Wei-Zhu , HONG Bi-Hong , ZHANG Yi-Ping , YI Rui-Zao . Synthesis of N-4-Pyridyl Amide Derivatives of N-Diisopropyloxyphosphoryl Amino Acids and Antidotal Activity of Tetrodotoxin (TTX)[J]. Chinese Journal of Organic Chemistry, 2012 , 32(01) : 178 -182 . DOI: 10.6023/cjoc1105102

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