Synthesis of combinatorial library of $\beta$-ketoacetoanilide chlorides and their antifungal activity against main plant pathogens

$\beta$-Ketoacetoanilide 염화물의 조합 라이브러리 합성 및 주요 식물병원균에 대한 항균활성

  • Hahn, Hoh-Gyu (Organic Chemistry, Lab, Korea Institute of Science and Technology) ;
  • Nam, Kee-Dal (Organic Chemistry, Lab, Korea Institute of Science and Technology) ;
  • Bae, Su-Yeal (Organic Chemistry, Lab, Korea Institute of Science and Technology) ;
  • Yang, Bum-Seung (Department of Chemistry, Kyonggi University) ;
  • Lee, Seon-Woo (Screening Division, Korea and Research Institute of Chemical Technology) ;
  • Cho, Kwang-Yun (Screening Division, Korea and Research Institute of Chemical Technology)
  • 한호규 (한국과학기술연구원 생체과학연구부) ;
  • 남기달 (한국과학기술연구원 생체과학연구부) ;
  • 배수열 (한국과학기술연구원 생체과학연구부) ;
  • 양범승 (경기대학교 화학과) ;
  • 이선우 (한국화학연구원 생물기능연구팀) ;
  • 조광연 (한국화학연구원 생물기능연구팀)
  • Published : 2004.03.30

Abstract

A synthesis of new $\beta$-ketoacetoanilide chloride derivatives and anti fungal activity of these compounds library against 6 typical plant pathogens were described. Reaction of ketene dimer with chlorine followed by treatment of aniline derivatives gave 89 kinds of the corresponding $\beta$-ketoacetoanilide chlorides through combinatorial synthetic technology using Carousel Reaction Stations. Evaluation of antifungal activity (in vivo) of this chemical library against rice blast, rice sheath blight, tomato aray mold, tomato late blight, wheat leaf rust and barley powdery mildew was carried out. In general, $\beta$-ketoacetoanilide chlorides which present a substituent at 4 in phenyl group(para) of the compounds showed selective control activity against tomato late blight caused by Phytophthora infestans.

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