"One-Pot"Synthesis and Antimalarial Activity of Formamidine Derivatives of 4-Anilinoquinoline

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概要

• 論文の詳細を見る

• Amodiaquine(AQ)is an antimalarial which is effective against chloroquino-resistant strains of Plasmodium falciparum but whose clinical use is severely restricted because of associated hepatotoxicity and agranulocytosis. "One-pot"synthesis of formamidines likely to be transformed into AQ derivatives is reported. Compared with AQ, the new compounds were devoid of in vitro cytotoxicity upon human embryonic lung cells and mouse peritoneal macrophages. One showed a potent in vivo activity in mice infected with P.berghei.Transformation of this compound by reductive amination led to a new type of AQ derivatives that displayed an in vitro activity similar to that of AQ but did not lead to toxic quinone-imines.

• 公益社団法人日本薬学会の論文
• 2001-08-01

著者

• Sergheraert C

  Institut De Biologie Et Institut Pasteur De Lille Faculte De Pharmacie Universite De Lille Ii.

• SERGHERAERT Christian

  Institut de Biologie et Institut Pasteur de Lille, UMR CNRS 8525, Universite de Lille 2

• Girault Sophie

  Institut De Biologie Et Institut Pasteur De Lille Faculte De Pharmacie Universite De Lille Ii.

• DELARUE Sandrine

  Institut de Biologie et Institut Pasteur de Lille, Faculte de Pharmacie, Universite de Lille II.

• DALI ALI

  Laboratoire de Biologie Parasitaire, IFR CNRN 63, Museum National d'Histoire Naturelle

• MAES Louis

  TIBOTEC, L11 General de Wittelaan

• GRELLIER Philippe

  Laboratoire de Biologie Parasitaire, IFR CNRN 63, Museum National d'Histoire Naturelle

• Grellier P

  Museum National D'histoire Naturelle Usm 0504

• Maes L

  Tibotec L11 General De Wittelaan

• Dali Ali

  Laboratoire De Biologie Parasitaire Ifr Cnrn 63 Museum National D'histoire Naturelle

• Delarue Sandrine

  Institut De Biologie Et Institut Pasteur De Lille Faculte De Pharmacie Universite De Lille Ii.

• Sergheraert Christian

  Institut De Biologie De Lille - Institut Pasteur De Lille - Ura Cnrs 1309

• Deli Ali

  Laboratoire de Biologie Parasitaire, IFR CNRN 63, Museum National d'Histoire Naturelle

• GRELLIER Philippe

  Laboratoire de Biologie Parasitaire, IFR CNRN 63, Museum National d'Histoire Naturelle

関連論文

• Novel N-(4-Piperidinyl)benzamide Antimalarials with Mammalian Protein Farnesyltransferase Inhibitory Activity
• "One-Pot"Synthesis and Antimalarial Activity of Formamidine Derivatives of 4-Anilinoquinoline
• A General Approach to the Synthesis of Polyamine Linked-Monoindolylmaleimides, a New Series of Trypanothione Reductase Inhibitors
• Identification of Inhibitors of an 80 kDa Protease from Trypanosoma cruzi through the Screening of a Combinatorial Peptide Library
• Compared Reactivities of Trypanothione and Glutathione in Conjugation Reactions

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