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논문 해외 국제전문학술지(SCI급) Phosphonamidate Compounds for Butyrylcholinesterase Selective Inhibitors

  • 학술지 구분 국제전문학술지(SCI급)
  • 게재년월 2020-12
  • 저자명 박정호
  • 학술지명 BULLETIN OF THE KOREAN CHEMICAL SOCIETY
  • 발행처명 WILEY-V C H VERLAG GMBH
  • 발행국가 해외
  • 논문언어 외국어
  • 전체저자수 5

논문 초록 (Abstract)

To find a new type of cholinergic drug, phosphonamidate compounds 18-32 were synthesized using a click reaction between propargylated-9,10-Dihydro-9-oxa-10-phosphaphenanthrene-10-oxide (DOPO, 2) and substituted benzyl azide. Their inhibitory activity against butyrylcholinesterase (BuChE) and acetylcholinesterase (AChE) was evaluated. Compound 31 was the most active of the 15 compounds (IC50 = 3.14 +/- 0.02 mu M for equine BuChE), whose IC50 value was slightly lower than the IC50 value of galantamine (IC50 = 9.4 +/- 2.50 for equine BuChE).