Piperazinyl quinolines as chemosensitizers to increase fluconazole susceptibility of Candida albicans clinical isolates
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Lindquist_Piperazinyl quinolines.pdf
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Author(s)
Youngsaye, Willmen
Vincent, Benjamin
Hartland, Cathy L.
Morgan, Barbara J.
Buhrlage, Sara J.
Johnston, Stephen
Bittker, Joshua A.
MacPherson, Lawrence
Dandapani, Sivaraman
Palmer, Michelle
Date Issued
June 2011
Journal
Bioorganic & Medicinal Chemistry Letters
Publisher
Elsevier
Citation
Youngsaye, Willmen, Benjamin Vincent, Cathy L. Hartland, Barbara J. Morgan, Sara J. Buhrlage, Stephen Johnston, Joshua A. Bittker, et al. “Piperazinyl Quinolines as Chemosensitizers to Increase Fluconazole Susceptibility of Candida Albicans Clinical Isolates.” Bioorganic & Medicinal Chemistry Letters 21, no. 18 (September 2011): 5502–5505.
Version
Author's final manuscript
Abstract
The effectiveness of the potent antifungal drug fluconazole is being compromised by the rise of drug-resistant fungal pathogens. While inhibition of Hsp90 or calcineurin can reverse drug resistance in Candida, such inhibitors also impair the homologous human host protein and fungal-selective chemosensitizers remain rare. The MLPCN library was screened to identify compounds that selectively reverse fluconazole resistance in a Candida albicans clinical isolate, while having no antifungal activity when administered as a single agent. A piperazinyl quinoline was identified as a new small-molecule probe (ML189) satisfying these criteria.
MIT Department
Massachusetts Institute of Technology. Department of Biology
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Creative Commons Attribution-Noncommercial-NoDerivatives
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DOI of Published Version
https://doi.org/10.1016/j.bmcl.2011.06.105
