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Bioorganic & medicinal chemistry letters DOI:10.1016/j.bmcl.2011.06.105

Piperazinyl quinolines as chemosensitizers to increase fluconazole susceptibility of Candida albicans clinical isolates.

Publication TypeJournal Article
Year of Publication2011
AuthorsYoungsaye, 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, Munoz, B
JournalBioorganic & medicinal chemistry letters
Volume21
Issue18
Pages5502-5
Date Published2011/09/15
ISSN0960-894X
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.

URLhttp://linkinghub.elsevier.com/retrieve/pii/S0960-894X(11)00896-1
DOI10.1016/j.bmcl.2011.06.105
Pubmed

http://www.ncbi.nlm.nih.gov/pubmed/21802942?dopt=Abstract