Abstract
Thein vitroactivities of the novel fungal Cyp51 inhibitor VT-1129 were evaluated against a large panel ofCryptococcus neoformansandCryptococcus gattiiisolates. VT-1129 demonstrated potent activities against bothCryptococcusspecies as demonstrated by low MIC50and MIC90values. ForC. gattii, thein vitropotency was maintained against all genotypes. In addition, significantly lower geometric mean MICs were observed for VT-1129 than for fluconazole againstC. neoformans, including isolates with reduced fluconazole susceptibility.
Copyright © 2016, American Society for Microbiology. All Rights Reserved.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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14-alpha Demethylase Inhibitors / chemical synthesis
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14-alpha Demethylase Inhibitors / pharmacology*
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Antifungal Agents / chemical synthesis
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Antifungal Agents / pharmacology*
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Cryptococcus gattii / drug effects
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Cryptococcus gattii / enzymology
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Cryptococcus gattii / genetics
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Cryptococcus neoformans / drug effects
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Cryptococcus neoformans / enzymology
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Cryptococcus neoformans / genetics
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Drug Resistance, Fungal / genetics
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Drugs, Investigational / chemical synthesis
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Drugs, Investigational / pharmacology*
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Fluconazole / pharmacology
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Fungal Proteins / antagonists & inhibitors*
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Fungal Proteins / genetics
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Fungal Proteins / metabolism
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Gene Expression
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Genotype
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Microbial Sensitivity Tests
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Pyridines / chemical synthesis
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Pyridines / pharmacology*
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Sterol 14-Demethylase / genetics
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Sterol 14-Demethylase / metabolism*
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Tetrazoles / chemical synthesis
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Tetrazoles / pharmacology*
Substances
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14-alpha Demethylase Inhibitors
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Antifungal Agents
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Drugs, Investigational
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Fungal Proteins
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Pyridines
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Tetrazoles
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VT-1129
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Fluconazole
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Sterol 14-Demethylase