論文

査読有り 責任著者
2007年

Antimalarial cation-dimers synthesized in two steps from an inexpensive starting material, isonicotinic acid

ChemMedChem
  • Kazunori Motoshima
  • ,
  • Yoshiko Hiwasa
  • ,
  • Mai Yoshikawa
  • ,
  • Kanji Fujimoto
  • ,
  • Akihiro Tai
  • ,
  • Hiroki Kakuta
  • ,
  • Kenji Sasaki

2
10
開始ページ
1527
終了ページ
1532
記述言語
英語
掲載種別
研究論文(学術雑誌)
DOI
10.1002/cmdc.200700107
出版者・発行元
WILEY-V C H VERLAG GMBH

Malaria is one of the three major serious infectious diseases in the world. As the area affected by malaria includes a large proportion of developing countries, there is a need for new antimalarials that can be synthesized and supplied inexpensively. To generate low-cost antimalarials, the MAP series 6-10, bis-cation dimers, synthesized by amidating the carboxyl group of isonicotinic acid (11) with various amines and by cationizing the nitrogen atoms of the pyridine ring with the corresponding alkyl bromides, were designed. This design enabled expansion of the structural variations of bis-cation-type antimalarial compounds. The compounds bearing alkyl or phenyl groups in the amide moieties showed remarkable antimalarial activities in vitro. Moreover, 1, 1'-(1, 12-dodecanediyl)bis[4-[(buthylamino)carbonyl]pyridinium bromide], MAP-412 (6d), exhibited a potent antimalarial activity (ED50 = 8.2 mg kg-(1)). Being prepared at low cost our biscation-type antimalarial compounds may be useful as lead compounds for inexpensive antimalarials.

リンク情報
DOI
https://doi.org/10.1002/cmdc.200700107
Web of Science
https://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=JSTA_CEL&SrcApp=J_Gate_JST&DestLinkType=FullRecord&KeyUT=WOS:000250283300014&DestApp=WOS_CPL
ID情報
  • DOI : 10.1002/cmdc.200700107
  • ISSN : 1860-7179
  • ORCIDのPut Code : 51294808
  • Web of Science ID : WOS:000250283300014

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