VFV as a New Effective CYP51 Structure-Derived Drug Candidate for Chagas Disease and Visceral Leishmaniasis

Sterol 14α-demethylases (CYP51) are the enzymes essential for sterol biosynthesis. They serve as clinical targets for antifungal azoles and are considered as targets for treatment of human Trypanosomatidae infections. Recently, we have shown that VNI, a potent and selective inhibitor of trypanosomal...

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Veröffentlicht in:	The Journal of infectious diseases 2015-11, Vol.212 (9), p.1439-1448
Hauptverfasser:	Lepesheva, Galina I., Hargrove, Tatiana Y., Rachakonda, Girish, Wawrzak, Zdzislaw, Pomel, Sébastien, Cojean, Sandrine, Nde, Pius N., Nes, W. David, Locuson, Charles W., Calcutt, M. Wade, Waterman, Michael R., Daniels, J. Scott, Loiseau, Philippe M., Villalta, Fernando
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antiprotozoal Agents - pharmacokinetics Antiprotozoal Agents - pharmacology Benzamides - pharmacokinetics Benzamides - pharmacology Biotransformation Chagas Disease - drug therapy Cytochrome P-450 Enzyme Inhibitors - pharmacokinetics Cytochrome P-450 Enzyme Inhibitors - pharmacology Cytochrome P-450 Enzyme System - chemistry Disease Models, Animal Female Humans Imidazoles - pharmacology Inhibitory Concentration 50 Leishmaniasis, Visceral - drug therapy Major and Brief Reports Mice Mice, Inbred BALB C Microsomes, Liver - drug effects Molecular Structure Oxadiazoles - pharmacokinetics Oxadiazoles - pharmacology PARASITES Rats Structure-Activity Relationship Tissue Distribution Trypanosoma cruzi - drug effects
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