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Novel N-(4-Piperidinyl)benzamide antimalarials with mammalian protein farnesyltransferase inhibitory activity.
Ryckebusch, Adina; Gilleron, Pauline; Millet, Régis; Houssin, Raymond; Lemoine, Amélie; Pommery, Nicole; Grellier, Philippe; Sergheraert, Christian; Hénichart, Jean-Pierre.
Affiliation
  • Ryckebusch A; Institut de Chimie Pharmaceutique Albert Lespagnol, EA 2692, Université de Lille 2, France.
Chem Pharm Bull (Tokyo) ; 53(10): 1324-6, 2005 Oct.
Article in En | MEDLINE | ID: mdl-16204993
Protein farnesyltransferase of Plasmodium falciparum is a potential target in the treatment of malaria for which increased drug resistance is observed. The design, synthesis and evaluation of a series of N-(4-piperidinyl)benzamides is reported. The most potent compounds showed in vitro activity against the parasite at submicromolar concentrations.
Subject(s)
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Collection: 01-internacional Database: MEDLINE Main subject: Benzamides / Alkyl and Aryl Transferases / Antimalarials Limits: Animals / Humans Language: En Journal: Chem Pharm Bull (Tokyo) Year: 2005 Document type: Article Affiliation country: France Country of publication: Japan
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Collection: 01-internacional Database: MEDLINE Main subject: Benzamides / Alkyl and Aryl Transferases / Antimalarials Limits: Animals / Humans Language: En Journal: Chem Pharm Bull (Tokyo) Year: 2005 Document type: Article Affiliation country: France Country of publication: Japan