Novel N-(4-Piperidinyl)benzamide Antimalarials with Mammalian Protein Farnesyltransferase Inhibitory Activity

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 agai...

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Veröffentlicht in:	Chemical & pharmaceutical bulletin 2005, Vol.53(10), pp.1324-1326
Hauptverfasser:	Ryckebusch, Adina, Gilleron, Pauline, Millet, Régis, Houssin, Raymond, Lemoine, Amélie, Pommery, Nicole, Grellier, Philippe, Sergheraert, Christian, Hénichart, Jean-Pierre
Format:	Artikel
Sprache:	eng
Schlagworte:	Alkyl and Aryl Transferases - antagonists & inhibitors Animals Antimalarials - chemical synthesis Antimalarials - chemistry Antimalarials - pharmacology Benzamides - chemical synthesis Benzamides - chemistry Benzamides - pharmacology Cell Line, Tumor Cell Proliferation - drug effects Chemical Sciences Drug Design Drug Evaluation, Preclinical Drug Screening Assays, Antitumor farnesyltransferase Humans inhibitor Life Sciences malaria Mice Microbiology and Parasitology Molecular Structure N-(4-piperidinyl)benzamide derivative Parasitic Sensitivity Tests Plasmodium falciparum Plasmodium falciparum - drug effects Plasmodium falciparum - enzymology Structure-Activity Relationship
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Zusammenfassung:	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.
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.53.1324