ML212: A small-molecule probe for investigating fluconazole resistance mechanisms in Candida albicans

The National Institutes of Health Molecular Libraries and Probe Production Centers Network (NIH-MLPCN) screened >300,000 compounds to evaluate their ability to restore fluconazole susceptibility in resistant Candida albicans isolates. Additional counter screens were incorporated to remove substan...

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Bibliographic Details
Published in:	Beilstein journal of organic chemistry Vol. 9; no. 1; pp. 1501 - 1507
Main Authors:	Youngsaye, Willmen, Hartland, Cathy L, Morgan, Barbara J, Ting, Amal, Nag, Partha P, Vincent, Benjamin, Mosher, Carrie A, Bittker, Joshua A, Dandapani, Sivaraman, Palmer, Michelle, Whitesell, Luke, Lindquist, Susan, Schreiber, Stuart L, Munoz, Benito
Format:	Journal Article
Language:	English
Published:	Germany Beilstein-Institut 26-07-2013
Subjects:	antifungal Candida albicans Chemistry chemosensitizer fluconazole Full Research Paper Molecular Libraries Probe Production Center Network (MLPCN) Candida albicans antifungal fluconazole chemosensitizer Molecular Libraries Probe Production Center Network (MLPCN)
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Summary:	The National Institutes of Health Molecular Libraries and Probe Production Centers Network (NIH-MLPCN) screened >300,000 compounds to evaluate their ability to restore fluconazole susceptibility in resistant Candida albicans isolates. Additional counter screens were incorporated to remove substances inherently toxic to either mammalian or fungal cells. A substituted indazole possessing the desired bioactivity profile was selected for further development, and initial investigation of structure-activity relationships led to the discovery of ML212.
ISSN:	1860-5397 1860-5397
DOI:	10.3762/bjoc.9.171