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Piperazinyl quinolines as chemosensitizers to increase fluconazole susceptibility of Candida albicans clinical isolates.
|Publication Type||Journal Article|
|Authors||Youngsaye, W., Vincent B., Hartland CL, Morgan BJ, Buhrlage SJ, Johnston S., Bittker JA, Macpherson L., Dandapani S., Palmer M., Whitesell L., Lindquist S., Schreiber SL, and Munoz B.|
|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.|
|Year of Publication||2011|
|Journal||Bioorganic & medicinal chemistry letters|
|Date Published (YYYY/MM/DD)||2011/09/15|