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Clinical Candidate VT-1161's Antiparasitic Effect In Vitro, Activity in a Murine Model of Chagas Disease, and Structural Characterization in Complex with the Target Enzyme CYP51 from Trypanosoma cruzi

A novel antifungal drug candidate, the 1-tetrazole-based agent VT-1161 [(R)-2-(2,4-difluorophenyl)-1,1-difluoro-3-(1H-tetrazol-1-yl)-1-{5-[4-(2,2,2-trifluoroethoxy)phenyl]pyridin-2-yl}propan-2-ol], which is currently in two phase 2b antifungal clinical trials, was found to be a tight-binding ligand...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Veröffentlicht in:Antimicrob Agents Chemother
Hauptverfasser: Hoekstra, William J., Hargrove, Tatiana Y., Wawrzak, Zdzislaw, da Gama Jaen Batista, Denise, da Silva, Cristiane F., Nefertiti, Aline S. G., Rachakonda, Girish, Schotzinger, Robert J., Villalta, Fernando, Soeiro, Maria de Nazaré C., Lepesheva, Galina I.
Format: Artigo
Sprache:Inglês
Veröffentlicht: American Society for Microbiology 2016
Schlagworte:
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4750653/
https://ncbi.nlm.nih.gov/pubmed/26643331
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1128/AAC.02287-15
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