In vitro and in vivo antimalarial activity of peptidomimetic protein farnesyltransferase inhibitors with improved membrane permeability

A series of ester derivatives of 17 with increased lipophilicity were synthesized and tested against P. falciparum in red blood cells, where the benzyl ester derivative 16 exhibited the best inhibition activity (ED 50 = 150 nM). Compound 16 showed in vivo antimalarial activity by 46.1% at a daily do...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2004-12, Vol.12 (24), p.6517-6526
Hauptverfasser:	Carrico, Dora, Ohkanda, Junko, Kendrick, Howard, Yokoyama, Kohei, Blaskovich, Michelle A., Bucher, Cynthia J., Buckner, Frederick S., Van Voorhis, Wesley C., Chakrabarti, Debopam, Croft, Simon L., Gelb, Michael H., Sebti, Saïd M., Hamilton, Andrew D.
Format:	Artikel
Sprache:	eng
Schlagworte:	Alkyl and Aryl Transferases - antagonists & inhibitors Animals Antibiotics. Antiinfectious agents. Antiparasitic agents Antimalarials - chemical synthesis Antimalarials - pharmacokinetics Antiparasitic agents Biological and medical sciences Cell Membrane Permeability Erythrocytes - parasitology Ester prodrug Esters - chemistry Farnesyltranstransferase Hydrophobic and Hydrophilic Interactions Malaria - drug therapy Medical sciences Mice Miscellaneous Molecular Mimicry NIH 3T3 Cells Peptides - chemical synthesis Peptides - pharmacokinetics Peptidomimetic Pharmacology. Drug treatments Plasmodium berghei - drug effects Plasmodium falciparum Plasmodium falciparum - drug effects Protein farnesyltransferase Structure-Activity Relationship
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